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  • 93
    Millipore canertinib
    Measuring of EGFR and c-erbB2 expression; activation of ERK1/2 and AKT in MCF-7, T47D, and their tamoxifen-resistant derivative cells MCF-7(TamR) and T47D (TamR) cells, respectively. (a) Changes in levels of total EGFR and c-erbB2 expression by Western blot. (b) Changes in levels of p-EGFR and p-c-erbB2 expression by Western blot. (c) Changes in levels of expression and activation of ERK1/2 and AKT by Western blot. (d) Changes in levels of EGFR expression and activation in t47d cells before and after the development of tamoxifen resistance by Western blot. (e) The inhibitory effects of <t>canertinib</t> on the activation of EGFR, Akt, and ERK1/2 and their encoded protein in both MCF-7 and MCF-7(TamR) cells by Western blot.
    Canertinib, supplied by Millipore, used in various techniques. Bioz Stars score: 93/100, based on 8 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Average 93 stars, based on 8 article reviews
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    93
    Selleck Chemicals canertinib
    Growth control graphs showing effect of selected HER-family TKIs in doubling concentrations on growth of breast cancer cell lines. ( a ) EGFR reversible inhibitor erlotinib. ( b ) Dual EGFR/HER2 reversible inhibitor lapatinib. ( c ) Pan-HER reversible inhibitor sapitinib. ( d ) Pan-HER irreversible inhibitor <t>canertinib.</t> ( e ) Pan-HER irreversible inhibitor afatinib. Sulforhodamine B colorimetric assay was used to determine the effect of treatment of breast cancer cell lines with doubling dilutions of HER-family inhibiting TKIs. The irreversible pan-inhibitors (e.g. afatinib, canertinib, neratinib) were consistently more effective than the reversible dual and pan inhibitors (e.g. lapatinib, sapitinib), which were in turn more effective than the reversible EGFR inhibitors (e.g. erlotinib, gefitinib). Each point is a representative of the mean ± SD of triplicate samples.
    Canertinib, supplied by Selleck Chemicals, used in various techniques. Bioz Stars score: 93/100, based on 56 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/canertinib/product/Selleck Chemicals
    Average 93 stars, based on 56 article reviews
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    88
    BioVision canertinib
    Modulation of PI3-K activity inversely impacts InlB-requirement for Lm entry in vitro. (A) Whole cell extracts from LS174T cells incubated with PBS or different concentrations of the <t>ErbB</t> inhibitor <t>CI-1033</t> (0.01, 0.1, or 1 µM) during 24 h, immunoblotted for P-Akt and total Akt. (B) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in LS174T cells incubated with PBS (controls, black bars) or CI-1033 1 µM (gray bars) for 24 h. (C) Whole cell extracts from LS174T cells incubated with PBS or CI-1033 1 µM and infected with WT Lm EGD and isogenic mutant Δ inlB , immunoblotted for P-Akt and total Akt. (D) Whole cell extracts from Jar cells incubated with PBS or EGF 50 ng/ml during 10, 30, or 60 min, immunoblotted for P-Akt and total Akt. (E) Whole cell extracts from Jar cells transfected with esiRNA PTEN, immunoblotted for PTEN. (F) Whole cell extracts from Jar cells transfected with esiRNA PTEN or control scrambled and incubated with PBS or EGF 50 ng/ml for 120 min, immunoblotted for P-Akt and total Akt. (G) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in Jar cells incubated with PBS, or transfected with esiRNA PTEN or incubated with EGF 50 ng/ml. (H) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in Jar cells incubated with PBS or incubated with EGF 50 ng/ml, and transfected with esiRNA PTEN. (B, G, and H) Invasion assays were performed in triplicates and represent at least three independent experiments for each condition tested. Relative entry represents the ratio of CFUs for each strain divided by the mean of CFUs for the WT Lm EGD strain. A one-way ANOVA test followed by a Bonferroni’s multiple comparisons was performed. Error bars, SEM. (A, C, D, E, and F) Immunoblots were performed at least two times. Densitometry was performed and the ratio of P-Akt over total Akt is relative to the PBS, for which the value is normalized to 1.
    Canertinib, supplied by BioVision, used in various techniques. Bioz Stars score: 88/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    85
    Pfizer Inc canertinib ci 1033
    Drug elution of T. brucei protein kinases using an ATP-affinity resin. Proteins in total cell lysate from T. brucei were bound on ATP resin. Sepharose 4B resin was used as control. Unbound proteins (Flow through) were recovered and resin was washed sequentially with buffer A and buffer A containing 1 M KCl (Panel A). Bound proteins were eluted with lapatinib (100 µM), or AEE788 (100 µM) or <t>canertinib</t> (100 µM) (Panel B, C and D, respectively). Proteins were visualized by silver staining. Matrix label, A is ATP-sepharose, and S is Sepharose 4B.
    Canertinib Ci 1033, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 85/100, based on 5 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Average 85 stars, based on 5 article reviews
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    90
    LC Laboratories ci 1033
    ErbB autocrine ligands in the EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of <t>CI-1033</t> cytotoxicity.
    Ci 1033, supplied by LC Laboratories, used in various techniques. Bioz Stars score: 90/100, based on 20 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    93
    Santa Cruz Biotechnology canertinib
    ErbB autocrine ligands in the EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of <t>CI-1033</t> cytotoxicity.
    Canertinib, supplied by Santa Cruz Biotechnology, used in various techniques. Bioz Stars score: 93/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/canertinib/product/Santa Cruz Biotechnology
    Average 93 stars, based on 3 article reviews
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    90
    Warner-Lambert canertinib
    ErbB autocrine ligands in the EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of <t>CI-1033</t> cytotoxicity.
    Canertinib, supplied by Warner-Lambert, used in various techniques. Bioz Stars score: 90/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/canertinib/product/Warner-Lambert
    Average 90 stars, based on 3 article reviews
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    canertinib - by Bioz Stars, 2020-08
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    90
    WuXi AppTec canertinib
    ErbB autocrine ligands in the EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of <t>CI-1033</t> cytotoxicity.
    Canertinib, supplied by WuXi AppTec, used in various techniques. Bioz Stars score: 90/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/canertinib/product/WuXi AppTec
    Average 90 stars, based on 2 article reviews
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    89
    Pfizer Inc treatment canertinib
    Dose dependent inhibition of sphere formation by anticancer drugs. To compare two sphere scoring parameters of the SSS vs. “number of spheres”, H1299 (2000 cells per well) were plated in 24-well ULA plates in TS medium supplemented with indicated drugs or vehicle for 4 days. %SSS i and %n i were then calculated. Concentration of drugs were as the following: (A) <t>CI-1033:</t> + 2 μM; (B) Erlotinib: + 3 μM, ++ 6 μM, +++ 10 μM; (C) MK2206: + 0.25 μM, ++ 0.5 μM, +++ 1 μM; (D) Perifosine: + 1 μM, ++ 3 μM, +++ 5 μM; and (E) BEZ235: + 25 nM, ++ 125 nM, +++ 250 nM. The results were presented as Mean ± SEM.
    Treatment Canertinib, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 89/100, based on 9 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    90
    Axon Medchem LLC canertinib
    Dose dependent inhibition of sphere formation by anticancer drugs. To compare two sphere scoring parameters of the SSS vs. “number of spheres”, H1299 (2000 cells per well) were plated in 24-well ULA plates in TS medium supplemented with indicated drugs or vehicle for 4 days. %SSS i and %n i were then calculated. Concentration of drugs were as the following: (A) <t>CI-1033:</t> + 2 μM; (B) Erlotinib: + 3 μM, ++ 6 μM, +++ 10 μM; (C) MK2206: + 0.25 μM, ++ 0.5 μM, +++ 1 μM; (D) Perifosine: + 1 μM, ++ 3 μM, +++ 5 μM; and (E) BEZ235: + 25 nM, ++ 125 nM, +++ 250 nM. The results were presented as Mean ± SEM.
    Canertinib, supplied by Axon Medchem LLC, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/canertinib/product/Axon Medchem LLC
    Average 90 stars, based on 1 article reviews
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    91
    AK Scientific canertinib
    Validation of selected GenEx-TNBC predictions in TNBC cell lines of multiple molecular subtypes Crystal violet staining of HCC1937 (BL1), BT549 (ML), and MDA-MB-453 (LAR) cells grown in the presence of the indicated concentrations of Mecamylamine (A) , <t>Canertinib</t> (B) , Bortezomib (C) , and Tretinoin (D) for seven (7) days. Data for each cell line were normalized to the appropriate solvent control (ethanol for Mecamylamine, DMSO for all others). Data were analyzed by two-way ANOVA with Tukey post hoc multiple comparisons test (asterisks indicate per-dose comparisons) and are presented as the mean +/− standard deviation (S.D.) for a single experiment performed with 6 technical replicates that is representative of at least two independent experiments (biological replicates).
    Canertinib, supplied by AK Scientific, used in various techniques. Bioz Stars score: 91/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    90
    LC Laboratories egf canertinib
    Validation of selected GenEx-TNBC predictions in TNBC cell lines of multiple molecular subtypes Crystal violet staining of HCC1937 (BL1), BT549 (ML), and MDA-MB-453 (LAR) cells grown in the presence of the indicated concentrations of Mecamylamine (A) , <t>Canertinib</t> (B) , Bortezomib (C) , and Tretinoin (D) for seven (7) days. Data for each cell line were normalized to the appropriate solvent control (ethanol for Mecamylamine, DMSO for all others). Data were analyzed by two-way ANOVA with Tukey post hoc multiple comparisons test (asterisks indicate per-dose comparisons) and are presented as the mean +/− standard deviation (S.D.) for a single experiment performed with 6 technical replicates that is representative of at least two independent experiments (biological replicates).
    Egf Canertinib, supplied by LC Laboratories, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    88
    LC Laboratories pan erbb inhibitor canertinib
    Validation of selected GenEx-TNBC predictions in TNBC cell lines of multiple molecular subtypes Crystal violet staining of HCC1937 (BL1), BT549 (ML), and MDA-MB-453 (LAR) cells grown in the presence of the indicated concentrations of Mecamylamine (A) , <t>Canertinib</t> (B) , Bortezomib (C) , and Tretinoin (D) for seven (7) days. Data for each cell line were normalized to the appropriate solvent control (ethanol for Mecamylamine, DMSO for all others). Data were analyzed by two-way ANOVA with Tukey post hoc multiple comparisons test (asterisks indicate per-dose comparisons) and are presented as the mean +/− standard deviation (S.D.) for a single experiment performed with 6 technical replicates that is representative of at least two independent experiments (biological replicates).
    Pan Erbb Inhibitor Canertinib, supplied by LC Laboratories, used in various techniques. Bioz Stars score: 88/100, based on 5 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/pan erbb inhibitor canertinib/product/LC Laboratories
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    84
    Selleck Chemicals canertinib inhibitor selleck chemicals cat
    Validation of selected GenEx-TNBC predictions in TNBC cell lines of multiple molecular subtypes Crystal violet staining of HCC1937 (BL1), BT549 (ML), and MDA-MB-453 (LAR) cells grown in the presence of the indicated concentrations of Mecamylamine (A) , <t>Canertinib</t> (B) , Bortezomib (C) , and Tretinoin (D) for seven (7) days. Data for each cell line were normalized to the appropriate solvent control (ethanol for Mecamylamine, DMSO for all others). Data were analyzed by two-way ANOVA with Tukey post hoc multiple comparisons test (asterisks indicate per-dose comparisons) and are presented as the mean +/− standard deviation (S.D.) for a single experiment performed with 6 technical replicates that is representative of at least two independent experiments (biological replicates).
    Canertinib Inhibitor Selleck Chemicals Cat, supplied by Selleck Chemicals, used in various techniques. Bioz Stars score: 84/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/canertinib inhibitor selleck chemicals cat/product/Selleck Chemicals
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    Image Search Results


    Measuring of EGFR and c-erbB2 expression; activation of ERK1/2 and AKT in MCF-7, T47D, and their tamoxifen-resistant derivative cells MCF-7(TamR) and T47D (TamR) cells, respectively. (a) Changes in levels of total EGFR and c-erbB2 expression by Western blot. (b) Changes in levels of p-EGFR and p-c-erbB2 expression by Western blot. (c) Changes in levels of expression and activation of ERK1/2 and AKT by Western blot. (d) Changes in levels of EGFR expression and activation in t47d cells before and after the development of tamoxifen resistance by Western blot. (e) The inhibitory effects of canertinib on the activation of EGFR, Akt, and ERK1/2 and their encoded protein in both MCF-7 and MCF-7(TamR) cells by Western blot.

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Measuring of EGFR and c-erbB2 expression; activation of ERK1/2 and AKT in MCF-7, T47D, and their tamoxifen-resistant derivative cells MCF-7(TamR) and T47D (TamR) cells, respectively. (a) Changes in levels of total EGFR and c-erbB2 expression by Western blot. (b) Changes in levels of p-EGFR and p-c-erbB2 expression by Western blot. (c) Changes in levels of expression and activation of ERK1/2 and AKT by Western blot. (d) Changes in levels of EGFR expression and activation in t47d cells before and after the development of tamoxifen resistance by Western blot. (e) The inhibitory effects of canertinib on the activation of EGFR, Akt, and ERK1/2 and their encoded protein in both MCF-7 and MCF-7(TamR) cells by Western blot.

    Article Snippet: Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Expressing, Activation Assay, Western Blot

    Chemical structure of canertinib (EGFR-irreversible tyrosine kinase inhibitor).

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Chemical structure of canertinib (EGFR-irreversible tyrosine kinase inhibitor).

    Article Snippet: Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques:

    Effect of EGFR inhibition with canertinib treatment on the sensitivity of MCF-7 and MCF-7(TamR) cells to a 48-hour treatment with (a) paclitaxel and (b) daunorubicin. Cells were subjected to a 48-hour cytotoxic treatment with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib before 4 days recovery in the same medium minus the cytotoxic. P values calculated from a paired t -test comparing growth inhibition between cells untreated with canertinib, both of which were treated with a given concentration of daunorubicin or paclitaxel. ∗ indicates p

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Effect of EGFR inhibition with canertinib treatment on the sensitivity of MCF-7 and MCF-7(TamR) cells to a 48-hour treatment with (a) paclitaxel and (b) daunorubicin. Cells were subjected to a 48-hour cytotoxic treatment with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib before 4 days recovery in the same medium minus the cytotoxic. P values calculated from a paired t -test comparing growth inhibition between cells untreated with canertinib, both of which were treated with a given concentration of daunorubicin or paclitaxel. ∗ indicates p

    Article Snippet: Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Inhibition, Concentration Assay

    Effect of EGFR inhibition with canertinib treatment on the sensitivity of (a) MCF-7 and (b) MCF-7(TamR) cells to carboplatin. Cells were subjected to a 9-day treatment with carboplatin with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib to the culture medium for the full length of the treatment, refreshed on day 5. P values calculated from a paired t -test comparing growth inhibition between cells treated with canertinib in addition to a given concentration of paclitaxel. ∗ indicates p

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Effect of EGFR inhibition with canertinib treatment on the sensitivity of (a) MCF-7 and (b) MCF-7(TamR) cells to carboplatin. Cells were subjected to a 9-day treatment with carboplatin with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib to the culture medium for the full length of the treatment, refreshed on day 5. P values calculated from a paired t -test comparing growth inhibition between cells treated with canertinib in addition to a given concentration of paclitaxel. ∗ indicates p

    Article Snippet: Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Inhibition, Concentration Assay

    Effect on growth of MCF-7 (red) and MCF-7(TamR) (blue) cells of a 9-day treatment of the EGFR inhibitors (a) canertinib and (b) canertinib added to the cell culture medium and refreshed on day 5 (test comparing growth inhibition between cell lines at a given concentration of EGFR inhibitor). ∗ indicates p

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Effect on growth of MCF-7 (red) and MCF-7(TamR) (blue) cells of a 9-day treatment of the EGFR inhibitors (a) canertinib and (b) canertinib added to the cell culture medium and refreshed on day 5 (test comparing growth inhibition between cell lines at a given concentration of EGFR inhibitor). ∗ indicates p

    Article Snippet: Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Cell Culture, Inhibition, Concentration Assay

    Measuring of EGFR and c-erbB2 expression; activation of ERK1/2 and AKT in MCF-7, T47D, and their tamoxifen-resistant derivative cells MCF-7(TamR) and T47D (TamR) cells, respectively. (a) Changes in levels of total EGFR and c-erbB2 expression by Western blot. (b) Changes in levels of p-EGFR and p-c-erbB2 expression by Western blot. (c) Changes in levels of expression and activation of ERK1/2 and AKT by Western blot. (d) Changes in levels of EGFR expression and activation in t47d cells before and after the development of tamoxifen resistance by Western blot. (e) The inhibitory effects of canertinib on the activation of EGFR, Akt, and ERK1/2 and their encoded protein in both MCF-7 and MCF-7(TamR) cells by Western blot.

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Measuring of EGFR and c-erbB2 expression; activation of ERK1/2 and AKT in MCF-7, T47D, and their tamoxifen-resistant derivative cells MCF-7(TamR) and T47D (TamR) cells, respectively. (a) Changes in levels of total EGFR and c-erbB2 expression by Western blot. (b) Changes in levels of p-EGFR and p-c-erbB2 expression by Western blot. (c) Changes in levels of expression and activation of ERK1/2 and AKT by Western blot. (d) Changes in levels of EGFR expression and activation in t47d cells before and after the development of tamoxifen resistance by Western blot. (e) The inhibitory effects of canertinib on the activation of EGFR, Akt, and ERK1/2 and their encoded protein in both MCF-7 and MCF-7(TamR) cells by Western blot.

    Article Snippet: Materials Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Expressing, Activation Assay, Western Blot

    Chemical structure of canertinib (EGFR-irreversible tyrosine kinase inhibitor).

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Chemical structure of canertinib (EGFR-irreversible tyrosine kinase inhibitor).

    Article Snippet: Materials Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques:

    Effect of EGFR inhibition with canertinib treatment on the sensitivity of MCF-7 and MCF-7(TamR) cells to a 48-hour treatment with (a) paclitaxel and (b) daunorubicin. Cells were subjected to a 48-hour cytotoxic treatment with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib before 4 days recovery in the same medium minus the cytotoxic. P values calculated from a paired t -test comparing growth inhibition between cells untreated with canertinib, both of which were treated with a given concentration of daunorubicin or paclitaxel. ∗ indicates p

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Effect of EGFR inhibition with canertinib treatment on the sensitivity of MCF-7 and MCF-7(TamR) cells to a 48-hour treatment with (a) paclitaxel and (b) daunorubicin. Cells were subjected to a 48-hour cytotoxic treatment with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib before 4 days recovery in the same medium minus the cytotoxic. P values calculated from a paired t -test comparing growth inhibition between cells untreated with canertinib, both of which were treated with a given concentration of daunorubicin or paclitaxel. ∗ indicates p

    Article Snippet: Materials Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Inhibition, Concentration Assay

    Effect of EGFR inhibition with canertinib treatment on the sensitivity of (a) MCF-7 and (b) MCF-7(TamR) cells to carboplatin. Cells were subjected to a 9-day treatment with carboplatin with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib to the culture medium for the full length of the treatment, refreshed on day 5. P values calculated from a paired t -test comparing growth inhibition between cells treated with canertinib in addition to a given concentration of paclitaxel. ∗ indicates p

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Effect of EGFR inhibition with canertinib treatment on the sensitivity of (a) MCF-7 and (b) MCF-7(TamR) cells to carboplatin. Cells were subjected to a 9-day treatment with carboplatin with the addition of (red) 0 μ M, (blue) 0.1 μ M, or (green) 1 μ M canertinib to the culture medium for the full length of the treatment, refreshed on day 5. P values calculated from a paired t -test comparing growth inhibition between cells treated with canertinib in addition to a given concentration of paclitaxel. ∗ indicates p

    Article Snippet: Materials Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Inhibition, Concentration Assay

    Effect on growth of MCF-7 (red) and MCF-7(TamR) (blue) cells of a 9-day treatment of the EGFR inhibitors (a) canertinib and (b) canertinib added to the cell culture medium and refreshed on day 5 (test comparing growth inhibition between cell lines at a given concentration of EGFR inhibitor). ∗ indicates p

    Journal: International Journal of Genomics

    Article Title: The Effect of Canertinib on Sensitivity of Cytotoxic Drugs in Tamoxifen-Resistant Breast Cancer Cells In Vitro

    doi: 10.1155/2018/7628734

    Figure Lengend Snippet: Effect on growth of MCF-7 (red) and MCF-7(TamR) (blue) cells of a 9-day treatment of the EGFR inhibitors (a) canertinib and (b) canertinib added to the cell culture medium and refreshed on day 5 (test comparing growth inhibition between cell lines at a given concentration of EGFR inhibitor). ∗ indicates p

    Article Snippet: Materials Clinical grade canertinib (CI-1033) and cytotoxic drugs (paclitaxel, etoposide, vinorelbine, and daunorubicin) were purchased from Sigma Chemical Co. (Sigma-Aldrich, Egypt).

    Techniques: Cell Culture, Inhibition, Concentration Assay

    Profile of EGFR tyrosine phosphorylation in cells pre-incubated with antioxidants or EGFR tyrosine kinase inhibitor and exposed to NBD compounds. MDA MB468 cells were pre-incubated with 0,2% DMSO ( a ) 500 U/ml PEG-catalase ( b ), 5 mM NAC ( c ), 5 mM thioglycerol ( d ) or 2 μM CI-1033 ( e ) and exposed to NBD compounds (100 μM), EGF (100 ng/ml) or vehicle for 15 min.

    Journal: Scientific Reports

    Article Title: Activation of EGFR by small compounds through coupling the generation of hydrogen peroxide to stable dimerization of Cu/Zn SOD1

    doi: 10.1038/srep21088

    Figure Lengend Snippet: Profile of EGFR tyrosine phosphorylation in cells pre-incubated with antioxidants or EGFR tyrosine kinase inhibitor and exposed to NBD compounds. MDA MB468 cells were pre-incubated with 0,2% DMSO ( a ) 500 U/ml PEG-catalase ( b ), 5 mM NAC ( c ), 5 mM thioglycerol ( d ) or 2 μM CI-1033 ( e ) and exposed to NBD compounds (100 μM), EGF (100 ng/ml) or vehicle for 15 min.

    Article Snippet: Catalase, PEG-catalase, thioglycerol, NAC, and compound CI-1033 were from Sigma-Aldrich.

    Techniques: Incubation, Multiple Displacement Amplification

    Dimerization of SOD1 in cancer cells exposed to lipophilic NBD compounds, and SOD1 exposed to NBD compounds in vitro . ( a ) Western blot analysis of proteins in MDA MB468 cells pre-incubated with NAC (5 mM), PEG-catalase (500 U/ml), thioglycerol (5 mM) or CI-1033 (2 μM) for 30 min, and then exposed to NBD compounds (100 μM) or EGF (500 ng/ml) for 15 min. SOD1 monomers were present in all cells (shown only in cells pre-incubated with DMSO). ( b ) Detection of NBD compounds bound to purified human SOD1 with Coomassie staining. ( c) Fluorescence detection of NBD compound/SOD1 complexes blotted onto NC membrane using a Typhoon 9410 scanner; the excitation wavelength was 488 nm and the emission wavelength was 526 nm.

    Journal: Scientific Reports

    Article Title: Activation of EGFR by small compounds through coupling the generation of hydrogen peroxide to stable dimerization of Cu/Zn SOD1

    doi: 10.1038/srep21088

    Figure Lengend Snippet: Dimerization of SOD1 in cancer cells exposed to lipophilic NBD compounds, and SOD1 exposed to NBD compounds in vitro . ( a ) Western blot analysis of proteins in MDA MB468 cells pre-incubated with NAC (5 mM), PEG-catalase (500 U/ml), thioglycerol (5 mM) or CI-1033 (2 μM) for 30 min, and then exposed to NBD compounds (100 μM) or EGF (500 ng/ml) for 15 min. SOD1 monomers were present in all cells (shown only in cells pre-incubated with DMSO). ( b ) Detection of NBD compounds bound to purified human SOD1 with Coomassie staining. ( c) Fluorescence detection of NBD compound/SOD1 complexes blotted onto NC membrane using a Typhoon 9410 scanner; the excitation wavelength was 488 nm and the emission wavelength was 526 nm.

    Article Snippet: Catalase, PEG-catalase, thioglycerol, NAC, and compound CI-1033 were from Sigma-Aldrich.

    Techniques: In Vitro, Western Blot, Multiple Displacement Amplification, Incubation, Purification, Staining, Fluorescence

    Effect of pan-ErbB inhibitors on NRG-1 action on human melanocytes and MelanoDerms. ( A ) HEM-DP were treated for 9 days with 50 ng/ml NRG-1 in the presence of C39 (0.5 μM) or CI-1033 (2 μM) or vehicle (DMSO) alone. The results are the average

    Journal: Journal of Cell Science

    Article Title: The fibroblast-derived paracrine factor neuregulin-1 has a novel role in regulating the constitutive color and melanocyte function in human skin

    doi: 10.1242/jcs.064774

    Figure Lengend Snippet: Effect of pan-ErbB inhibitors on NRG-1 action on human melanocytes and MelanoDerms. ( A ) HEM-DP were treated for 9 days with 50 ng/ml NRG-1 in the presence of C39 (0.5 μM) or CI-1033 (2 μM) or vehicle (DMSO) alone. The results are the average

    Article Snippet: For the experiments where the MelanoDerms were treated with NRG-1 and/or various pan-ErbB inhibitors, the dark MelanoDerms were first incubated with a pan-ErbB inhibitor (0.5 μM C39, EMD Chemicals, Gibbistown, NJ or 2 μM CI-1033, Selleck Chemicals LLC, US) for 30 minutes or with vehicle (DMSO) only before treatment with 50 ng/ml NRG-1; identical amounts of DMSO (0.02%) were added to all samples.

    Techniques:

    Canertinib toxicity in zebrafish. Lateral line hair cells were quantified and compared among different groups. Data plotted as means +/− standard error of the mean (SEM). Neomycin was used as a positive control (Neo 200 μM), while dimethyl

    Journal: Hearing research

    Article Title: Canertinib–Induces Ototoxicity in Three Preclinical Models

    doi: 10.1016/j.heares.2015.07.002

    Figure Lengend Snippet: Canertinib toxicity in zebrafish. Lateral line hair cells were quantified and compared among different groups. Data plotted as means +/− standard error of the mean (SEM). Neomycin was used as a positive control (Neo 200 μM), while dimethyl

    Article Snippet: After canertinib exposure, larvae were anesthetized with MS-222 (3-aminobenzoic acid ethyl ester, methanesulfonate salt; Sigma-Aldrich) and then fixed for 1 hr in 4% paraformaldehyde (PFA) at room temperature.

    Techniques: Positive Control

    Two canertinib treatment cycles for C57BL/6J and CBA/CaJ mice. Timeline of functional and histological assays and canertinib treatments.

    Journal: Hearing research

    Article Title: Canertinib–Induces Ototoxicity in Three Preclinical Models

    doi: 10.1016/j.heares.2015.07.002

    Figure Lengend Snippet: Two canertinib treatment cycles for C57BL/6J and CBA/CaJ mice. Timeline of functional and histological assays and canertinib treatments.

    Article Snippet: After canertinib exposure, larvae were anesthetized with MS-222 (3-aminobenzoic acid ethyl ester, methanesulfonate salt; Sigma-Aldrich) and then fixed for 1 hr in 4% paraformaldehyde (PFA) at room temperature.

    Techniques: Crocin Bleaching Assay, Mouse Assay, Functional Assay

    Loss of hair cells after canertinib treatment. The same C57BL/6J mice were used for histological quantification of hair cells. Hair cell counts were graphically displayed for both the control (A) and canertinib-treated (B) mice from apex to base (the

    Journal: Hearing research

    Article Title: Canertinib–Induces Ototoxicity in Three Preclinical Models

    doi: 10.1016/j.heares.2015.07.002

    Figure Lengend Snippet: Loss of hair cells after canertinib treatment. The same C57BL/6J mice were used for histological quantification of hair cells. Hair cell counts were graphically displayed for both the control (A) and canertinib-treated (B) mice from apex to base (the

    Article Snippet: After canertinib exposure, larvae were anesthetized with MS-222 (3-aminobenzoic acid ethyl ester, methanesulfonate salt; Sigma-Aldrich) and then fixed for 1 hr in 4% paraformaldehyde (PFA) at room temperature.

    Techniques: Mouse Assay

    Hearing changes in C57BL/6J mice after canertinib treatment. ABR threshold shifts of C57BL/6J mice after the first (A) and second (B) cycle of the treatment. Control mice (red diamond; 3 males and 4 females) are compared to the drug-treated mice (blue

    Journal: Hearing research

    Article Title: Canertinib–Induces Ototoxicity in Three Preclinical Models

    doi: 10.1016/j.heares.2015.07.002

    Figure Lengend Snippet: Hearing changes in C57BL/6J mice after canertinib treatment. ABR threshold shifts of C57BL/6J mice after the first (A) and second (B) cycle of the treatment. Control mice (red diamond; 3 males and 4 females) are compared to the drug-treated mice (blue

    Article Snippet: After canertinib exposure, larvae were anesthetized with MS-222 (3-aminobenzoic acid ethyl ester, methanesulfonate salt; Sigma-Aldrich) and then fixed for 1 hr in 4% paraformaldehyde (PFA) at room temperature.

    Techniques: Mouse Assay

    Growth control graphs showing effect of selected HER-family TKIs in doubling concentrations on growth of breast cancer cell lines. ( a ) EGFR reversible inhibitor erlotinib. ( b ) Dual EGFR/HER2 reversible inhibitor lapatinib. ( c ) Pan-HER reversible inhibitor sapitinib. ( d ) Pan-HER irreversible inhibitor canertinib. ( e ) Pan-HER irreversible inhibitor afatinib. Sulforhodamine B colorimetric assay was used to determine the effect of treatment of breast cancer cell lines with doubling dilutions of HER-family inhibiting TKIs. The irreversible pan-inhibitors (e.g. afatinib, canertinib, neratinib) were consistently more effective than the reversible dual and pan inhibitors (e.g. lapatinib, sapitinib), which were in turn more effective than the reversible EGFR inhibitors (e.g. erlotinib, gefitinib). Each point is a representative of the mean ± SD of triplicate samples.

    Journal: Scientific Reports

    Article Title: Synergistic effects of various Her inhibitors in combination with IGF-1R, C-MET and Src targeting agents in breast cancer cell lines

    doi: 10.1038/s41598-017-04301-8

    Figure Lengend Snippet: Growth control graphs showing effect of selected HER-family TKIs in doubling concentrations on growth of breast cancer cell lines. ( a ) EGFR reversible inhibitor erlotinib. ( b ) Dual EGFR/HER2 reversible inhibitor lapatinib. ( c ) Pan-HER reversible inhibitor sapitinib. ( d ) Pan-HER irreversible inhibitor canertinib. ( e ) Pan-HER irreversible inhibitor afatinib. Sulforhodamine B colorimetric assay was used to determine the effect of treatment of breast cancer cell lines with doubling dilutions of HER-family inhibiting TKIs. The irreversible pan-inhibitors (e.g. afatinib, canertinib, neratinib) were consistently more effective than the reversible dual and pan inhibitors (e.g. lapatinib, sapitinib), which were in turn more effective than the reversible EGFR inhibitors (e.g. erlotinib, gefitinib). Each point is a representative of the mean ± SD of triplicate samples.

    Article Snippet: Lapatinib, sapitinib, canertinib, neratinib, imatinib and dasatinib were all acquired from Selleckchem (USA).

    Techniques: Colorimetric Assay

    HPV8E6 directly binds to the ubiquitinated EGFR in an UV-dependent manner. (A) RTS3b cells were transiently transfected with a vector directing the expression of FLAG-tagged HPV8E6 under control of the CMV-promoter or the empty vector. Where indicated the cells have been irradiated with UV-light 30 min prior harvesting. 400 μg of extracts were incubated with the anti-EGFR-antibody (lanes 1–4) or with the FLAG-antibody (lanes 5–8), both coupled to sepharose, washed four times in 0.3 M KCl-buffer prior analysis by WB and 40 μg of the extracts were used in the input blots. (B) IP with anti-EGFR sepharose and 800 μg of extracts derived from the stable RTS3b-pLXSN and RTS3b-HPV8E6 lines, either left untreated or UV-irradiated 30 min prior harvesting. FLAG-HPV8E6 and EGFR present in the precipitate as well as in the input were detected by WB. (C) Extracts from UV-irradiated RTS3b cells that have been transiently transfected with the FLAG-HPV8E6 or the FLAG-vector were incubated either with DMSO (lanes 1, 2, 5), 3 μM (lane 3) or 7 μM (lane 4) Canertinib for 30 min. The IP was performed with the FLAG-antibody. All WB were developed with the indicated antibodies. In lanes 6–10, C33A cells were transiently transfected with expression vectors for EGFR-GFP and FLAG-HPV8E6, and UV-irradiated, where indicated, prior harvesting 30 min later. EGFR-GFP was precipitated from 400 μg of extract by the EGFR antibody and bound HPV8E6 was detected by the FLAG-antibody. The input blots were developed with the antibodies against pEGFR-Y1068, GFP, and FLAG. The positions of the molecular weight markers are provided (in kDa).

    Journal: Frontiers in Microbiology

    Article Title: Induction of Tyrosine Phosphorylation of UV-Activated EGFR by the Beta-Human Papillomavirus Type 8 E6 Leads to Papillomatosis

    doi: 10.3389/fmicb.2017.02197

    Figure Lengend Snippet: HPV8E6 directly binds to the ubiquitinated EGFR in an UV-dependent manner. (A) RTS3b cells were transiently transfected with a vector directing the expression of FLAG-tagged HPV8E6 under control of the CMV-promoter or the empty vector. Where indicated the cells have been irradiated with UV-light 30 min prior harvesting. 400 μg of extracts were incubated with the anti-EGFR-antibody (lanes 1–4) or with the FLAG-antibody (lanes 5–8), both coupled to sepharose, washed four times in 0.3 M KCl-buffer prior analysis by WB and 40 μg of the extracts were used in the input blots. (B) IP with anti-EGFR sepharose and 800 μg of extracts derived from the stable RTS3b-pLXSN and RTS3b-HPV8E6 lines, either left untreated or UV-irradiated 30 min prior harvesting. FLAG-HPV8E6 and EGFR present in the precipitate as well as in the input were detected by WB. (C) Extracts from UV-irradiated RTS3b cells that have been transiently transfected with the FLAG-HPV8E6 or the FLAG-vector were incubated either with DMSO (lanes 1, 2, 5), 3 μM (lane 3) or 7 μM (lane 4) Canertinib for 30 min. The IP was performed with the FLAG-antibody. All WB were developed with the indicated antibodies. In lanes 6–10, C33A cells were transiently transfected with expression vectors for EGFR-GFP and FLAG-HPV8E6, and UV-irradiated, where indicated, prior harvesting 30 min later. EGFR-GFP was precipitated from 400 μg of extract by the EGFR antibody and bound HPV8E6 was detected by the FLAG-antibody. The input blots were developed with the antibodies against pEGFR-Y1068, GFP, and FLAG. The positions of the molecular weight markers are provided (in kDa).

    Article Snippet: The Canertinib group was administered once 20 mg/kg Canertinib (CI-1033, Selleckchem, S1019) solved in 150 μl PBS by gavage and the control group obtained 150 μl PBS 4 h prior UV-irradiation.

    Techniques: Transfection, Plasmid Preparation, Expressing, Irradiation, Incubation, Western Blot, Derivative Assay, Molecular Weight

    Inhibition of the RTK-activity of the EGFR by the pan-ErbB-inhibitor Canertinib (CI-1033) suppresses UV-induced papillomatosis in K14-HPV8E6 transgenic mice. (A) Immunohistochemical staining of paraffin embedded sections obtained from skin of K14-HPV8E6 transgenic mice 13 days after UV-exposure with the anti-pEGFR-Y1068 or rabbit IgG isotype control (magnification 1:400). (B) Transgenic mice obtained either Canertinib (CI-1033) (20 mg/kg weight) or the same volume of PBS 4 h prior UV-irradiation followed by applications of Canertinib once daily at a dose of 10 mg/kg weight or 150 μl PBS for 24 days, as given in the time line. The pictures represent examples of the lesions from four mice treated with CI-1033 (M19, 20, 23, and M26) and from one control mouse which obtained PBS (M22). The graph beneath shows the quantification of RT-PCR results with RNA isolated from two PBS and three Canertinib-treated animals to demonstrate the expression of HPV8E6. (C) Histology with H/E staining of skin section obtained from two PBS-control (M21 and M22) and four Canertinib (CI-1033)-treated animals (M19, M20, M23, and M26) 24 days after UV-irradiation.

    Journal: Frontiers in Microbiology

    Article Title: Induction of Tyrosine Phosphorylation of UV-Activated EGFR by the Beta-Human Papillomavirus Type 8 E6 Leads to Papillomatosis

    doi: 10.3389/fmicb.2017.02197

    Figure Lengend Snippet: Inhibition of the RTK-activity of the EGFR by the pan-ErbB-inhibitor Canertinib (CI-1033) suppresses UV-induced papillomatosis in K14-HPV8E6 transgenic mice. (A) Immunohistochemical staining of paraffin embedded sections obtained from skin of K14-HPV8E6 transgenic mice 13 days after UV-exposure with the anti-pEGFR-Y1068 or rabbit IgG isotype control (magnification 1:400). (B) Transgenic mice obtained either Canertinib (CI-1033) (20 mg/kg weight) or the same volume of PBS 4 h prior UV-irradiation followed by applications of Canertinib once daily at a dose of 10 mg/kg weight or 150 μl PBS for 24 days, as given in the time line. The pictures represent examples of the lesions from four mice treated with CI-1033 (M19, 20, 23, and M26) and from one control mouse which obtained PBS (M22). The graph beneath shows the quantification of RT-PCR results with RNA isolated from two PBS and three Canertinib-treated animals to demonstrate the expression of HPV8E6. (C) Histology with H/E staining of skin section obtained from two PBS-control (M21 and M22) and four Canertinib (CI-1033)-treated animals (M19, M20, M23, and M26) 24 days after UV-irradiation.

    Article Snippet: The Canertinib group was administered once 20 mg/kg Canertinib (CI-1033, Selleckchem, S1019) solved in 150 μl PBS by gavage and the control group obtained 150 μl PBS 4 h prior UV-irradiation.

    Techniques: Inhibition, Activity Assay, Transgenic Assay, Mouse Assay, Immunohistochemistry, Staining, Irradiation, Reverse Transcription Polymerase Chain Reaction, Isolation, Expressing

    Selection of canertinib resistant cells. Tu-2449 cells were treated with canertinib for 10 days. The drug was replenished in the growth medium in 24 hour intervals by half-medium change. After 10 days, drug treatment was discontinued for three days. Cell growth was microscopically monitored after 1, 3, 5, 7, 9 and 13 days. The upper panel shows different fields while the lower panel shows the same field. Magnification, 40×. Drug treatment selects for small cell colonies with higher cell density.

    Journal: MedChemComm

    Article Title: Tumor cell resistance against targeted therapeutics: the density of cultured glioma tumor cells enhances Stat3 activity and offers protection against the tyrosine kinase inhibitor canertinib cell resistance against targeted therapeutics: the density of cultured glioma tumor cells enhances Stat3 activity and offers protection against the tyrosine kinase inhibitor canertinib †The authors declare no conflict of interest.

    doi: 10.1039/c6md00463f

    Figure Lengend Snippet: Selection of canertinib resistant cells. Tu-2449 cells were treated with canertinib for 10 days. The drug was replenished in the growth medium in 24 hour intervals by half-medium change. After 10 days, drug treatment was discontinued for three days. Cell growth was microscopically monitored after 1, 3, 5, 7, 9 and 13 days. The upper panel shows different fields while the lower panel shows the same field. Magnification, 40×. Drug treatment selects for small cell colonies with higher cell density.

    Article Snippet: Chemicals The tyrosine kinase inhibitor canertinib (CI-1033) was purchased from SelleckChem, Munich, Germany, dissolved in sterile dimethyl sulfoxide (DMSO) and stored at –80 °C.

    Techniques: Selection

    Selected canertinib resistant colonies become sensitive again to drug treatment when cultured at low cell densities. Parental and 5 selected colonies of Tu-2449 glioma cells were plated at low densities (comparable to Fig. 2 panel one) and treated with 5 μM canertinib or only the growth medium. The drug was replenished in the growth medium in 24 hour intervals. Cell viability was monitored after 24, 48 and 72 h using the AlamarBlue® assay. Repeated addition of 5 μM canertinib significantly reduced the cell viability in all analyzed cell clones after 72 h. Results are presented as mean ± SD, with respect to 72 h untreated cells; **** p

    Journal: MedChemComm

    Article Title: Tumor cell resistance against targeted therapeutics: the density of cultured glioma tumor cells enhances Stat3 activity and offers protection against the tyrosine kinase inhibitor canertinib cell resistance against targeted therapeutics: the density of cultured glioma tumor cells enhances Stat3 activity and offers protection against the tyrosine kinase inhibitor canertinib †The authors declare no conflict of interest.

    doi: 10.1039/c6md00463f

    Figure Lengend Snippet: Selected canertinib resistant colonies become sensitive again to drug treatment when cultured at low cell densities. Parental and 5 selected colonies of Tu-2449 glioma cells were plated at low densities (comparable to Fig. 2 panel one) and treated with 5 μM canertinib or only the growth medium. The drug was replenished in the growth medium in 24 hour intervals. Cell viability was monitored after 24, 48 and 72 h using the AlamarBlue® assay. Repeated addition of 5 μM canertinib significantly reduced the cell viability in all analyzed cell clones after 72 h. Results are presented as mean ± SD, with respect to 72 h untreated cells; **** p

    Article Snippet: Chemicals The tyrosine kinase inhibitor canertinib (CI-1033) was purchased from SelleckChem, Munich, Germany, dissolved in sterile dimethyl sulfoxide (DMSO) and stored at –80 °C.

    Techniques: Cell Culture, Alamar Blue Assay, Clone Assay

    Canertinib treatment of Tu-2449 glioma cells induces the arrest of cell growth after 24 h and prolonged inhibition causes cell death dependent upon exposure time and drug dose. (A) Tu-2449 cells were treated with a single dose of 5 or 10 μM canertinib or DMSO and cultured for 24 h. Microscopic monitoring after 24 h reveals growth arrest in canertinib treated cells; scale bar: 100 μm. (B) Tu-2449 cells were treated with canertinib or DMSO and the drug was replenished in the growth medium in 24 hour intervals. Cell viability was monitored after 24, 48 and 72 h using the AlamarBlue® assay. Repeated addition of canertinib arrests the cells and causes cell death after 24 h (10 μM canertinib) or 48 h (5 μM canertinib). Results are presented as mean ± SD, expressed as a percentage with respect to 72 h DMSO. ns = not significant, **** p

    Journal: MedChemComm

    Article Title: Tumor cell resistance against targeted therapeutics: the density of cultured glioma tumor cells enhances Stat3 activity and offers protection against the tyrosine kinase inhibitor canertinib cell resistance against targeted therapeutics: the density of cultured glioma tumor cells enhances Stat3 activity and offers protection against the tyrosine kinase inhibitor canertinib †The authors declare no conflict of interest.

    doi: 10.1039/c6md00463f

    Figure Lengend Snippet: Canertinib treatment of Tu-2449 glioma cells induces the arrest of cell growth after 24 h and prolonged inhibition causes cell death dependent upon exposure time and drug dose. (A) Tu-2449 cells were treated with a single dose of 5 or 10 μM canertinib or DMSO and cultured for 24 h. Microscopic monitoring after 24 h reveals growth arrest in canertinib treated cells; scale bar: 100 μm. (B) Tu-2449 cells were treated with canertinib or DMSO and the drug was replenished in the growth medium in 24 hour intervals. Cell viability was monitored after 24, 48 and 72 h using the AlamarBlue® assay. Repeated addition of canertinib arrests the cells and causes cell death after 24 h (10 μM canertinib) or 48 h (5 μM canertinib). Results are presented as mean ± SD, expressed as a percentage with respect to 72 h DMSO. ns = not significant, **** p

    Article Snippet: Chemicals The tyrosine kinase inhibitor canertinib (CI-1033) was purchased from SelleckChem, Munich, Germany, dissolved in sterile dimethyl sulfoxide (DMSO) and stored at –80 °C.

    Techniques: Inhibition, Cell Culture, Alamar Blue Assay

    Modulation of PI3-K activity inversely impacts InlB-requirement for Lm entry in vitro. (A) Whole cell extracts from LS174T cells incubated with PBS or different concentrations of the ErbB inhibitor CI-1033 (0.01, 0.1, or 1 µM) during 24 h, immunoblotted for P-Akt and total Akt. (B) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in LS174T cells incubated with PBS (controls, black bars) or CI-1033 1 µM (gray bars) for 24 h. (C) Whole cell extracts from LS174T cells incubated with PBS or CI-1033 1 µM and infected with WT Lm EGD and isogenic mutant Δ inlB , immunoblotted for P-Akt and total Akt. (D) Whole cell extracts from Jar cells incubated with PBS or EGF 50 ng/ml during 10, 30, or 60 min, immunoblotted for P-Akt and total Akt. (E) Whole cell extracts from Jar cells transfected with esiRNA PTEN, immunoblotted for PTEN. (F) Whole cell extracts from Jar cells transfected with esiRNA PTEN or control scrambled and incubated with PBS or EGF 50 ng/ml for 120 min, immunoblotted for P-Akt and total Akt. (G) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in Jar cells incubated with PBS, or transfected with esiRNA PTEN or incubated with EGF 50 ng/ml. (H) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in Jar cells incubated with PBS or incubated with EGF 50 ng/ml, and transfected with esiRNA PTEN. (B, G, and H) Invasion assays were performed in triplicates and represent at least three independent experiments for each condition tested. Relative entry represents the ratio of CFUs for each strain divided by the mean of CFUs for the WT Lm EGD strain. A one-way ANOVA test followed by a Bonferroni’s multiple comparisons was performed. Error bars, SEM. (A, C, D, E, and F) Immunoblots were performed at least two times. Densitometry was performed and the ratio of P-Akt over total Akt is relative to the PBS, for which the value is normalized to 1.

    Journal: The Journal of Experimental Medicine

    Article Title: PI3-kinase activation is critical for host barrier permissiveness to Listeria monocytogenes

    doi: 10.1084/jem.20141406

    Figure Lengend Snippet: Modulation of PI3-K activity inversely impacts InlB-requirement for Lm entry in vitro. (A) Whole cell extracts from LS174T cells incubated with PBS or different concentrations of the ErbB inhibitor CI-1033 (0.01, 0.1, or 1 µM) during 24 h, immunoblotted for P-Akt and total Akt. (B) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in LS174T cells incubated with PBS (controls, black bars) or CI-1033 1 µM (gray bars) for 24 h. (C) Whole cell extracts from LS174T cells incubated with PBS or CI-1033 1 µM and infected with WT Lm EGD and isogenic mutant Δ inlB , immunoblotted for P-Akt and total Akt. (D) Whole cell extracts from Jar cells incubated with PBS or EGF 50 ng/ml during 10, 30, or 60 min, immunoblotted for P-Akt and total Akt. (E) Whole cell extracts from Jar cells transfected with esiRNA PTEN, immunoblotted for PTEN. (F) Whole cell extracts from Jar cells transfected with esiRNA PTEN or control scrambled and incubated with PBS or EGF 50 ng/ml for 120 min, immunoblotted for P-Akt and total Akt. (G) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in Jar cells incubated with PBS, or transfected with esiRNA PTEN or incubated with EGF 50 ng/ml. (H) Invasion assays of WT Lm EGD and isogenic mutants Δ inlA and Δ inlB in Jar cells incubated with PBS or incubated with EGF 50 ng/ml, and transfected with esiRNA PTEN. (B, G, and H) Invasion assays were performed in triplicates and represent at least three independent experiments for each condition tested. Relative entry represents the ratio of CFUs for each strain divided by the mean of CFUs for the WT Lm EGD strain. A one-way ANOVA test followed by a Bonferroni’s multiple comparisons was performed. Error bars, SEM. (A, C, D, E, and F) Immunoblots were performed at least two times. Densitometry was performed and the ratio of P-Akt over total Akt is relative to the PBS, for which the value is normalized to 1.

    Article Snippet: The pan-ErbB inhibitor CI-1033 was purchased from Biovision.

    Techniques: Activity Assay, In Vitro, Incubation, Infection, Mutagenesis, Transfection, esiRNA, Western Blot

    Drug elution of T. brucei protein kinases using an ATP-affinity resin. Proteins in total cell lysate from T. brucei were bound on ATP resin. Sepharose 4B resin was used as control. Unbound proteins (Flow through) were recovered and resin was washed sequentially with buffer A and buffer A containing 1 M KCl (Panel A). Bound proteins were eluted with lapatinib (100 µM), or AEE788 (100 µM) or canertinib (100 µM) (Panel B, C and D, respectively). Proteins were visualized by silver staining. Matrix label, A is ATP-sepharose, and S is Sepharose 4B.

    Journal: PLoS ONE

    Article Title: Lapatinib-Binding Protein Kinases in the African Trypanosome: Identification of Cellular Targets for Kinase-Directed Chemical Scaffolds

    doi: 10.1371/journal.pone.0056150

    Figure Lengend Snippet: Drug elution of T. brucei protein kinases using an ATP-affinity resin. Proteins in total cell lysate from T. brucei were bound on ATP resin. Sepharose 4B resin was used as control. Unbound proteins (Flow through) were recovered and resin was washed sequentially with buffer A and buffer A containing 1 M KCl (Panel A). Bound proteins were eluted with lapatinib (100 µM), or AEE788 (100 µM) or canertinib (100 µM) (Panel B, C and D, respectively). Proteins were visualized by silver staining. Matrix label, A is ATP-sepharose, and S is Sepharose 4B.

    Article Snippet: AEE788 (Novartis) inhibits EGFR and VEGFR , , and canertinib (CI-1033) (Pfizer) is a pan-inhibitor of EGFRs – .

    Techniques: Flow Cytometry, Silver Staining

    Lapatinib, AEE788 and canertinib kill bloodstream T. brucei . Bloodstream form T. brucei (initial cell density of 2×10 3 cells/ml) were cultured in 24-well plates for 48 h with either DMSO (control) or different concentrations of drug. Cells were counted with a hemocytometer and the graphs plotted. Data are mean ± standard deviation obtained from two independent experiments performed in duplicate. ( A ). Effect of lapatinib on growth of T. brucei . ( B ). Comparison of growth inhibitory effect of lapatinib on T. brucei to HeLa cells. HeLa and T. brucei cells were cultured for 48 h with variable concentrations of lapatinib. Relative cell density represents the live cells expressed as percentages of the control ( i.e. , DMSO-treated) experiment. ( C ) Trypanosome kill assay. Time-course of trypanocidal effect of lapatinib. Trypanosomes (10 6 cells/ml) were treated with DMSO (solvent) or lapatinib (10 µM) for 8 h: viable cells were counted every hour, and plotted for each time point.

    Journal: PLoS ONE

    Article Title: Lapatinib-Binding Protein Kinases in the African Trypanosome: Identification of Cellular Targets for Kinase-Directed Chemical Scaffolds

    doi: 10.1371/journal.pone.0056150

    Figure Lengend Snippet: Lapatinib, AEE788 and canertinib kill bloodstream T. brucei . Bloodstream form T. brucei (initial cell density of 2×10 3 cells/ml) were cultured in 24-well plates for 48 h with either DMSO (control) or different concentrations of drug. Cells were counted with a hemocytometer and the graphs plotted. Data are mean ± standard deviation obtained from two independent experiments performed in duplicate. ( A ). Effect of lapatinib on growth of T. brucei . ( B ). Comparison of growth inhibitory effect of lapatinib on T. brucei to HeLa cells. HeLa and T. brucei cells were cultured for 48 h with variable concentrations of lapatinib. Relative cell density represents the live cells expressed as percentages of the control ( i.e. , DMSO-treated) experiment. ( C ) Trypanosome kill assay. Time-course of trypanocidal effect of lapatinib. Trypanosomes (10 6 cells/ml) were treated with DMSO (solvent) or lapatinib (10 µM) for 8 h: viable cells were counted every hour, and plotted for each time point.

    Article Snippet: AEE788 (Novartis) inhibits EGFR and VEGFR , , and canertinib (CI-1033) (Pfizer) is a pan-inhibitor of EGFRs – .

    Techniques: Cell Culture, Standard Deviation

    Chemical structure of lapatinib, AEE788, and canertinib.

    Journal: PLoS ONE

    Article Title: Lapatinib-Binding Protein Kinases in the African Trypanosome: Identification of Cellular Targets for Kinase-Directed Chemical Scaffolds

    doi: 10.1371/journal.pone.0056150

    Figure Lengend Snippet: Chemical structure of lapatinib, AEE788, and canertinib.

    Article Snippet: AEE788 (Novartis) inhibits EGFR and VEGFR , , and canertinib (CI-1033) (Pfizer) is a pan-inhibitor of EGFRs – .

    Techniques:

    Best models of TbLBPK•drug complexes are consistent with affinity chromatography elution data. ( A ) Predicted ICM binding scores of lapatinib (red), AEE788 (green) and canertinib (magenta) in the binding pockets of the protein kinases. The dotted line represents a hypothetical cutoff for kinase elution by drug after an NAD + wash of the affinity column. ( B ) Predicted binding poses for lapatinib (red), AEE788 (green) and canertinib (magenta) to their highest affinity protein kinases; TbLBPK1, TbLBPK2, and TbCBPK1, respectively. Kinase hinge region is shown in ribbon, ligand atom placement surface is represented by a wire mesh and colored according to its binding properties.

    Journal: PLoS ONE

    Article Title: Lapatinib-Binding Protein Kinases in the African Trypanosome: Identification of Cellular Targets for Kinase-Directed Chemical Scaffolds

    doi: 10.1371/journal.pone.0056150

    Figure Lengend Snippet: Best models of TbLBPK•drug complexes are consistent with affinity chromatography elution data. ( A ) Predicted ICM binding scores of lapatinib (red), AEE788 (green) and canertinib (magenta) in the binding pockets of the protein kinases. The dotted line represents a hypothetical cutoff for kinase elution by drug after an NAD + wash of the affinity column. ( B ) Predicted binding poses for lapatinib (red), AEE788 (green) and canertinib (magenta) to their highest affinity protein kinases; TbLBPK1, TbLBPK2, and TbCBPK1, respectively. Kinase hinge region is shown in ribbon, ligand atom placement surface is represented by a wire mesh and colored according to its binding properties.

    Article Snippet: AEE788 (Novartis) inhibits EGFR and VEGFR , , and canertinib (CI-1033) (Pfizer) is a pan-inhibitor of EGFRs – .

    Techniques: Affinity Chromatography, Binding Assay, Affinity Column

    (A–C) DNA synthesis assay. DNA synthesis was determined by incorporation of [ 3 H]thymidine into mesothelioma cells. Different drugs (A, ZD1839; B, OSI-774; C, CI-1033) and/or TGF-α (12.5 ng/ml) were added and cells incubated for 48 hours. The results are expressed as counts per minute (cpm) and presented as the mean ± SD triplicates for each TGF-α and/or drug concentrations.

    Journal: Neoplasia (New York, N.Y.)

    Article Title: Inhibition of Proliferation, Migration, and Matrix Metalloprotease Production in Malignant Mesothelioma Cells by Tyrosine Kinase Inhibitors 1

    doi:

    Figure Lengend Snippet: (A–C) DNA synthesis assay. DNA synthesis was determined by incorporation of [ 3 H]thymidine into mesothelioma cells. Different drugs (A, ZD1839; B, OSI-774; C, CI-1033) and/or TGF-α (12.5 ng/ml) were added and cells incubated for 48 hours. The results are expressed as counts per minute (cpm) and presented as the mean ± SD triplicates for each TGF-α and/or drug concentrations.

    Article Snippet: OSI-774 was provided by OSI/Genentech (Melville, NY) and CI-1033 was provided by Pfizer (New York, NY).

    Techniques: DNA Synthesis, Incubation

    Induction of early-stage apoptosis by TK inhibitors in malignant mesothelioma cells. The apoptosis was determined by Annexin-V FITC and PI staining and analyzed by flow cytometry. Histograms of cells versus log fluorescence intensity were generated. Shaded histograms represent fluorescence of cells treated with TGF-α only; open histograms indicate fluorescence of cells treated with different drugs and TGF-α. The early stage of apoptosis was observed in 14%, 28%, and 30% of the ZL34 cells treated with 10 µM of ZD1839, OSI-774, and CI-1033, respectively. Data shown are representative of three independent experiments. For each sample, 10,000 cells were analyzed.

    Journal: Neoplasia (New York, N.Y.)

    Article Title: Inhibition of Proliferation, Migration, and Matrix Metalloprotease Production in Malignant Mesothelioma Cells by Tyrosine Kinase Inhibitors 1

    doi:

    Figure Lengend Snippet: Induction of early-stage apoptosis by TK inhibitors in malignant mesothelioma cells. The apoptosis was determined by Annexin-V FITC and PI staining and analyzed by flow cytometry. Histograms of cells versus log fluorescence intensity were generated. Shaded histograms represent fluorescence of cells treated with TGF-α only; open histograms indicate fluorescence of cells treated with different drugs and TGF-α. The early stage of apoptosis was observed in 14%, 28%, and 30% of the ZL34 cells treated with 10 µM of ZD1839, OSI-774, and CI-1033, respectively. Data shown are representative of three independent experiments. For each sample, 10,000 cells were analyzed.

    Article Snippet: OSI-774 was provided by OSI/Genentech (Melville, NY) and CI-1033 was provided by Pfizer (New York, NY).

    Techniques: Staining, Flow Cytometry, Cytometry, Fluorescence, Generated

    ErbB autocrine ligands in the EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of CI-1033 cytotoxicity.

    Journal: Biotechnology and bioengineering

    Article Title: A Multivariate Model of ErbB Network Composition Predicts Ovarian Cancer Cell Response to Canertinib

    doi: 10.1002/bit.23297

    Figure Lengend Snippet: ErbB autocrine ligands in the EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of CI-1033 cytotoxicity.

    Article Snippet: To our knowledge, the sensitivity of these cell lines to CI-1033 has not been reported.

    Techniques:

    Top nine reduced models. ( A ) Subsets of proteins used in the top nine models, shaded box indicates the protein was included in the X matrix. ( B ) Representative predictions of a reduced CI-1033 cytotoxicity model (X matrix composed of ErbB1, NRG1-β,

    Journal: Biotechnology and bioengineering

    Article Title: A Multivariate Model of ErbB Network Composition Predicts Ovarian Cancer Cell Response to Canertinib

    doi: 10.1002/bit.23297

    Figure Lengend Snippet: Top nine reduced models. ( A ) Subsets of proteins used in the top nine models, shaded box indicates the protein was included in the X matrix. ( B ) Representative predictions of a reduced CI-1033 cytotoxicity model (X matrix composed of ErbB1, NRG1-β,

    Article Snippet: To our knowledge, the sensitivity of these cell lines to CI-1033 has not been reported.

    Techniques:

    Ovarian cancer cell lines show different sensitivities to CI-1033

    Journal: Biotechnology and bioengineering

    Article Title: A Multivariate Model of ErbB Network Composition Predicts Ovarian Cancer Cell Response to Canertinib

    doi: 10.1002/bit.23297

    Figure Lengend Snippet: Ovarian cancer cell lines show different sensitivities to CI-1033

    Article Snippet: To our knowledge, the sensitivity of these cell lines to CI-1033 has not been reported.

    Techniques:

    A multi-protein model is needed to predict cell line cytotoxicity to CI-1033. ( A ) Full PLSR model of CI-1033 cytotoxicity, and ( B ) reduced CI-1033 cytotoxicity models built using subsets of proteins. N/A indicates inability to build a model using that

    Journal: Biotechnology and bioengineering

    Article Title: A Multivariate Model of ErbB Network Composition Predicts Ovarian Cancer Cell Response to Canertinib

    doi: 10.1002/bit.23297

    Figure Lengend Snippet: A multi-protein model is needed to predict cell line cytotoxicity to CI-1033. ( A ) Full PLSR model of CI-1033 cytotoxicity, and ( B ) reduced CI-1033 cytotoxicity models built using subsets of proteins. N/A indicates inability to build a model using that

    Article Snippet: To our knowledge, the sensitivity of these cell lines to CI-1033 has not been reported.

    Techniques:

    Representative CI-1033 cytotoxicity dose-response curves. ( A ) OVCAR5, ( B ) OVCA433.

    Journal: Biotechnology and bioengineering

    Article Title: A Multivariate Model of ErbB Network Composition Predicts Ovarian Cancer Cell Response to Canertinib

    doi: 10.1002/bit.23297

    Figure Lengend Snippet: Representative CI-1033 cytotoxicity dose-response curves. ( A ) OVCAR5, ( B ) OVCA433.

    Article Snippet: To our knowledge, the sensitivity of these cell lines to CI-1033 has not been reported.

    Techniques:

    Expression of ErbB1-4 in EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of CI-1033 cytotoxicity.

    Journal: Biotechnology and bioengineering

    Article Title: A Multivariate Model of ErbB Network Composition Predicts Ovarian Cancer Cell Response to Canertinib

    doi: 10.1002/bit.23297

    Figure Lengend Snippet: Expression of ErbB1-4 in EOC cell lines in the prediction set. The grey box represents the data range included in the original full PLSR model of CI-1033 cytotoxicity.

    Article Snippet: To our knowledge, the sensitivity of these cell lines to CI-1033 has not been reported.

    Techniques: Expressing

    Dose dependent inhibition of sphere formation by anticancer drugs. To compare two sphere scoring parameters of the SSS vs. “number of spheres”, H1299 (2000 cells per well) were plated in 24-well ULA plates in TS medium supplemented with indicated drugs or vehicle for 4 days. %SSS i and %n i were then calculated. Concentration of drugs were as the following: (A) CI-1033: + 2 μM; (B) Erlotinib: + 3 μM, ++ 6 μM, +++ 10 μM; (C) MK2206: + 0.25 μM, ++ 0.5 μM, +++ 1 μM; (D) Perifosine: + 1 μM, ++ 3 μM, +++ 5 μM; and (E) BEZ235: + 25 nM, ++ 125 nM, +++ 250 nM. The results were presented as Mean ± SEM.

    Journal: PLoS ONE

    Article Title: A Reliable Parameter to Standardize the Scoring of Stem Cell Spheres

    doi: 10.1371/journal.pone.0127348

    Figure Lengend Snippet: Dose dependent inhibition of sphere formation by anticancer drugs. To compare two sphere scoring parameters of the SSS vs. “number of spheres”, H1299 (2000 cells per well) were plated in 24-well ULA plates in TS medium supplemented with indicated drugs or vehicle for 4 days. %SSS i and %n i were then calculated. Concentration of drugs were as the following: (A) CI-1033: + 2 μM; (B) Erlotinib: + 3 μM, ++ 6 μM, +++ 10 μM; (C) MK2206: + 0.25 μM, ++ 0.5 μM, +++ 1 μM; (D) Perifosine: + 1 μM, ++ 3 μM, +++ 5 μM; and (E) BEZ235: + 25 nM, ++ 125 nM, +++ 250 nM. The results were presented as Mean ± SEM.

    Article Snippet: Drugs and treatment Canertinib (CI-1033, Pfizer Pharmaceuticals) and Erlotinib (Selleck Chemicals) were kindly provided by Dr. Mukesh Nyati at University of Michigan.

    Techniques: Inhibition, Concentration Assay

    Validation of selected GenEx-TNBC predictions in TNBC cell lines of multiple molecular subtypes Crystal violet staining of HCC1937 (BL1), BT549 (ML), and MDA-MB-453 (LAR) cells grown in the presence of the indicated concentrations of Mecamylamine (A) , Canertinib (B) , Bortezomib (C) , and Tretinoin (D) for seven (7) days. Data for each cell line were normalized to the appropriate solvent control (ethanol for Mecamylamine, DMSO for all others). Data were analyzed by two-way ANOVA with Tukey post hoc multiple comparisons test (asterisks indicate per-dose comparisons) and are presented as the mean +/− standard deviation (S.D.) for a single experiment performed with 6 technical replicates that is representative of at least two independent experiments (biological replicates).

    Journal: Oncotarget

    Article Title: Differential prioritization of therapies to subtypes of triple negative breast cancer using a systems medicine method

    doi: 10.18632/oncotarget.21669

    Figure Lengend Snippet: Validation of selected GenEx-TNBC predictions in TNBC cell lines of multiple molecular subtypes Crystal violet staining of HCC1937 (BL1), BT549 (ML), and MDA-MB-453 (LAR) cells grown in the presence of the indicated concentrations of Mecamylamine (A) , Canertinib (B) , Bortezomib (C) , and Tretinoin (D) for seven (7) days. Data for each cell line were normalized to the appropriate solvent control (ethanol for Mecamylamine, DMSO for all others). Data were analyzed by two-way ANOVA with Tukey post hoc multiple comparisons test (asterisks indicate per-dose comparisons) and are presented as the mean +/− standard deviation (S.D.) for a single experiment performed with 6 technical replicates that is representative of at least two independent experiments (biological replicates).

    Article Snippet: Compounds Mecamylamine (Sigma Aldrich), Canertinib (AK Scientific, Union City, CA), Bortezomib (AK Scientific), Tretinoin (AK Scientific), and AMG900 (Selleckchem, Houston, TX) were resuspended in dimethyl sulfoxide (DMSO – Canertinib, Bortezomib, Tretinoin, AMG900) or 200 proof ethanol (EtOH – Mecamylamine) at a concentration of 10 mM, stored at -20°C, and used at the indicated concentrations.

    Techniques: Staining, Multiple Displacement Amplification, Standard Deviation