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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 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/canertinib ci 1033/product/Pfizer Inc
Average 85 stars, based on 1 article reviews
Price from $9.99 to $1999.99
canertinib ci 1033 - by Bioz Stars, 2020-09
85/100 stars

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1) Product Images from "Lapatinib-Binding Protein Kinases in the African Trypanosome: Identification of Cellular Targets for Kinase-Directed Chemical Scaffolds"

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

Journal: PLoS ONE

doi: 10.1371/journal.pone.0056150

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.
Figure Legend 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.

Techniques Used: 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.
Figure Legend 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.

Techniques Used: Cell Culture, Standard Deviation

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

Techniques Used:

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.
Figure Legend 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.

Techniques Used: Affinity Chromatography, Binding Assay, Affinity Column

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    Pfizer Inc ci 1033
    (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, <t>CI-1033)</t> 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.
    Ci 1033, supplied by Pfizer Inc, used in various techniques. Bioz Stars score: 90/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Average 90 stars, based on 3 article reviews
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    ci 1033 - by Bioz Stars, 2020-09
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    (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

    CI-1033 selectively inhibits the proliferation of NF1 MPNST cell lines. On day 0, plates were treated with either vehicle or the indicated concentration of CI-1033. Cells were harvested and counted using the Trypan Blue exclusion assay. These data show

    Journal:

    Article Title: Suppression of Proliferation of Two Independent NF1 Malignant Peripheral Nerve Sheath Tumor Cell Lines by the pan-ErbB Inhibitor CI-1033

    doi:

    Figure Lengend Snippet: CI-1033 selectively inhibits the proliferation of NF1 MPNST cell lines. On day 0, plates were treated with either vehicle or the indicated concentration of CI-1033. Cells were harvested and counted using the Trypan Blue exclusion assay. These data show

    Article Snippet: In contrast, concentrations of CI-1033 up to 1 μM did not markedly affect the proliferation of the non-NF1 STS-26T line ( ).

    Techniques: Concentration Assay, Trypan Blue Exclusion Assay

    CI-1033 inhibits the proliferation of NF1 but not the non-NF1 MPNST line in 5% serum

    Journal:

    Article Title: Suppression of Proliferation of Two Independent NF1 Malignant Peripheral Nerve Sheath Tumor Cell Lines by the pan-ErbB Inhibitor CI-1033

    doi:

    Figure Lengend Snippet: CI-1033 inhibits the proliferation of NF1 but not the non-NF1 MPNST line in 5% serum

    Article Snippet: In contrast, concentrations of CI-1033 up to 1 μM did not markedly affect the proliferation of the non-NF1 STS-26T line ( ).

    Techniques:

    Inhibition of ErbB receptor activation reverses GSK3β inhibition in vitro and in vivo . A , Representative blots showing the dose–response effects of the ErbB inhibitor CI-1033 in blocking EGF-induced activity of ErbB in SH-SY5Y cells. EGF-induced

    Journal: The Journal of Neuroscience

    Article Title: Interplay between Cyclin-Dependent Kinase 5 and Glycogen Synthase Kinase 3β Mediated by Neuregulin Signaling Leads to Differential Effects on Tau Phosphorylation and Amyloid Precursor Protein Processing

    doi: 10.1523/JNEUROSCI.5245-07.2008

    Figure Lengend Snippet: Inhibition of ErbB receptor activation reverses GSK3β inhibition in vitro and in vivo . A , Representative blots showing the dose–response effects of the ErbB inhibitor CI-1033 in blocking EGF-induced activity of ErbB in SH-SY5Y cells. EGF-induced

    Article Snippet: CI-1033 at the indicated concentration was added to the culture 2 h before epidermal growth factor (EGF) treatment.

    Techniques: Inhibition, Activation Assay, In Vitro, In Vivo, Blocking Assay, Activity Assay