oral multitarget tyrosine kinase inhibitor cm082  (MultiTarget Pharmaceuticals)

Journal: Molecular Therapy Oncolytics

Article Title: Vorolanib, a novel tyrosine receptor kinase receptor inhibitor with potent preclinical anti-angiogenic and anti-tumor activity

doi: 10.1016/j.omto.2022.01.001

Figure Lengend Snippet: IC 50 values of competitive binding between vorolanib (CM082) and sunitinib with different kinases

Article Snippet: The binding of the compounds including, vorolanib (CM082) and sunitinib (as the control), with 287 kinases covering about 55% of the predicted human protein kinome, was tested using the KINOMEscan assay (Ambit Biosciences, San Diego, CA).

Techniques: Binding Assay

Journal: Molecular Therapy Oncolytics

Article Title: Vorolanib, a novel tyrosine receptor kinase receptor inhibitor with potent preclinical anti-angiogenic and anti-tumor activity

doi: 10.1016/j.omto.2022.01.001

Figure Lengend Snippet: IC 50 values of vorolanib (CM082) on human umbilical vein endothelial cell proliferation with or without VEGF165

Article Snippet: The binding of the compounds including, vorolanib (CM082) and sunitinib (as the control), with 287 kinases covering about 55% of the predicted human protein kinome, was tested using the KINOMEscan assay (Ambit Biosciences, San Diego, CA).

Techniques:

Journal: Molecular Therapy Oncolytics

Article Title: Vorolanib, a novel tyrosine receptor kinase receptor inhibitor with potent preclinical anti-angiogenic and anti-tumor activity

doi: 10.1016/j.omto.2022.01.001

Figure Lengend Snippet: IC 50 values of vorolanib for different cancer cell lines

Article Snippet: The binding of the compounds including, vorolanib (CM082) and sunitinib (as the control), with 287 kinases covering about 55% of the predicted human protein kinome, was tested using the KINOMEscan assay (Ambit Biosciences, San Diego, CA).

Techniques:

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology and FFA results of CNV modeling. (a) Histology of CNV lesions stained with HE shows that CNV formation and broke the Brunch's membrane at 21 days after photocoagulation. Dome-like CNV complexes, consisting of fibrovascular tissue, retinal pigment epithelial cells, and pigment clumps, are shown and white arrow indicates the vessel lumina of neovascular. (b) FFA results showed fluorescein leakage of CNV in each group at day 14, 21, and 28 (7 days after CM082 treatment) separately. The signal intensity of capillary in background region was defined as “0” whereas the signal intensity of the main branch of the retinal vein was defined as “1”. (c) There is no significant difference between the intensity score of leakage in each group at day 14, 21, and 28 ( p > 0.05). Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques: Staining, Membrane

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Distribution of CM082 and its metabolites in plasma and eye tissues. (a, b, and c) The concentrations (ng/ml or ng/g) of CM082, X-297, and X-471 in plasma and ocular tissues ( n = 9). There is no significant difference between the concentration of CM082 in plasma and eyes. The same is true for X-297. However, the concentration of X471 in eyes (OS: 16.68 ± 2.18, OD: 15.82 ± 1.85) is obviously lower than that in plasma (32.04 ± 4.57) ( ∗∗ p < 0.01). (d, e, and f) The concentration of CM082, X-297, and X-471 was detected in different ocular tissues ( n = 9). There is no significant difference in concentration of CM082, X-297, and X-471 between OS and OD.

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques: Clinical Proteomics, Concentration Assay

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: FFA results of the CM082 (10 mg/kg/d) group and the corresponding vehicle-treated group at different time points. (a, b; n = 10) FFA showed that the leakage of fluorescein at laser spots are at nearly same extent in vehicle-treated and CM082 group 7 days after laser injury ( p > 0.05, n = 9). (c, d) Leakage of fluorescein in the CM082-treated group was reduced at 21 days after laser injury ( ∗∗ p < 0.01, n = 9).

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques:

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology examine stained with HE of the CM082 (10 mg/kg/d) group ( n = 2) and the corresponding vehicle group ( n = 2) was obtained after FFA examination at day 7, 14, and 21. (a, b) Results showed a smaller CNV size of the CM082-treated group at day14 and 21. CNV complexes consist of retinal pigment epithelial cells, pigment clumps, and vascular tufts were observed. The CNV under CM082 treated was thinner in the center compared with that in the vehicle-treated group. Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques: Staining

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: FFA results of the CM082 (30 mg/kg/d)-treated group and the corresponding dose of the vehicle-treated group at different time points. Results of FFA showed the leakage of fluorescein at laser spots in vehicle-treated and CM082 group 7 (a, b; n = 10), 14 (c, d; n = 9), and 21 (e, f; n = 8) days after laser injury. (g, h, and i) The fluorescence signal intensity of CM082-treated group was statistically lower than the vehicle-treated group at 14 days and 21 days ( ∗∗∗ p < 0.001). (j) The signal intensity at 14 and 21 days was obviously lower than that at 7 days in the CM082 group ( ∗∗∗ p < 0.001).

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques: Fluorescence

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology of CNV lesions stained with hematoxylin-eosin of the CM082 (30 mg/kg) group ( n = 6) and the corresponding dose of the vehicle group ( n = 6) was obtained after FFA examination. Results showed that administration of CM082 reduces laser-induced CNV lesions. (a) In the vehicle-treated group, CNV formed and broke the Brunch's membrane. The depigmentation in RPE, aggregation of macrophage, and neovascularization were obtained 14 days and 21 days after photocoagulation. (b) In the CM082 group, the edema, depigmentation, and CNV areas significantly decreased comparing to vehicle-treated group at the same time point. Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques: Staining, Membrane

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Immunohistochemical analysis of the CM082 (30 mg/kg) group and the corresponding dose of the vehicle group. (a, n = 3) The result of immunohistochemical stain with p-VEGFR-2 in the vehicle-treated group at 7, 14 and 21, days after laser photocoagulated. There are large numbers of yellow granules distributed in vessels, outer plexiform layer, and RPE layer. (b, n = 3) The expression of p-VEGFR-2 in each structure in the CM082-treated group was significantly lower than the control group at the same time point. Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques: Immunohistochemical staining, Staining, Expressing, Control

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Representative CNV lesions in RPE-choroid-sclera flat mounts by perfusion of fluorescein isothiocyanate-dextrcan were obtained 7, 14, and 21 days after photocoagulation. (a, b) The areas of CNV lesions in the vehicle-treated and CM082 group at day 7 were shown and without statistical difference. CM082 (or vehicle) was delivered orally from day 7 ( n = 3). The area of CNV lesions was significantly reduced under CM082 treatment at day 14 (c, d; n = 3) and 21 (e, f; n = 3). (h, i) There is a significantly inhibition of CNV area in CM082 group compared with that in vehicle-treated group ( ∗∗ p < 0.01, ∗∗∗ p < 0.001). (j) The CNV area in the CM082 group showed a regression at day 14 and 21 compared with that in day 7 ( ∗ p < 0.05). Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical study of X-82 (CM082) in the USA and is currently conducting a randomized phase 2b study in patients with exudative AMD [ ] ( NCT02348359 ).

Techniques: Inhibition

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology and FFA results of CNV modeling. (a) Histology of CNV lesions stained with HE shows that CNV formation and broke the Brunch's membrane at 21 days after photocoagulation. Dome-like CNV complexes, consisting of fibrovascular tissue, retinal pigment epithelial cells, and pigment clumps, are shown and white arrow indicates the vessel lumina of neovascular. (b) FFA results showed fluorescein leakage of CNV in each group at day 14, 21, and 28 (7 days after CM082 treatment) separately. The signal intensity of capillary in background region was defined as “0” whereas the signal intensity of the main branch of the retinal vein was defined as “1”. (c) There is no significant difference between the intensity score of leakage in each group at day 14, 21, and 28 ( p > 0.05). Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques: Staining, Membrane

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Distribution of CM082 and its metabolites in plasma and eye tissues. (a, b, and c) The concentrations (ng/ml or ng/g) of CM082, X-297, and X-471 in plasma and ocular tissues ( n = 9). There is no significant difference between the concentration of CM082 in plasma and eyes. The same is true for X-297. However, the concentration of X471 in eyes (OS: 16.68 ± 2.18, OD: 15.82 ± 1.85) is obviously lower than that in plasma (32.04 ± 4.57) ( ∗∗ p < 0.01). (d, e, and f) The concentration of CM082, X-297, and X-471 was detected in different ocular tissues ( n = 9). There is no significant difference in concentration of CM082, X-297, and X-471 between OS and OD.

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques: Clinical Proteomics, Concentration Assay

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: FFA results of the CM082 (10 mg/kg/d) group and the corresponding vehicle-treated group at different time points. (a, b; n = 10) FFA showed that the leakage of fluorescein at laser spots are at nearly same extent in vehicle-treated and CM082 group 7 days after laser injury ( p > 0.05, n = 9). (c, d) Leakage of fluorescein in the CM082-treated group was reduced at 21 days after laser injury ( ∗∗ p < 0.01, n = 9).

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques:

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology examine stained with HE of the CM082 (10 mg/kg/d) group ( n = 2) and the corresponding vehicle group ( n = 2) was obtained after FFA examination at day 7, 14, and 21. (a, b) Results showed a smaller CNV size of the CM082-treated group at day14 and 21. CNV complexes consist of retinal pigment epithelial cells, pigment clumps, and vascular tufts were observed. The CNV under CM082 treated was thinner in the center compared with that in the vehicle-treated group. Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques: Staining

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: FFA results of the CM082 (30 mg/kg/d)-treated group and the corresponding dose of the vehicle-treated group at different time points. Results of FFA showed the leakage of fluorescein at laser spots in vehicle-treated and CM082 group 7 (a, b; n = 10), 14 (c, d; n = 9), and 21 (e, f; n = 8) days after laser injury. (g, h, and i) The fluorescence signal intensity of CM082-treated group was statistically lower than the vehicle-treated group at 14 days and 21 days ( ∗∗∗ p < 0.001). (j) The signal intensity at 14 and 21 days was obviously lower than that at 7 days in the CM082 group ( ∗∗∗ p < 0.001).

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques: Fluorescence

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology of CNV lesions stained with hematoxylin-eosin of the CM082 (30 mg/kg) group ( n = 6) and the corresponding dose of the vehicle group ( n = 6) was obtained after FFA examination. Results showed that administration of CM082 reduces laser-induced CNV lesions. (a) In the vehicle-treated group, CNV formed and broke the Brunch's membrane. The depigmentation in RPE, aggregation of macrophage, and neovascularization were obtained 14 days and 21 days after photocoagulation. (b) In the CM082 group, the edema, depigmentation, and CNV areas significantly decreased comparing to vehicle-treated group at the same time point. Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques: Staining, Membrane

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Immunohistochemical analysis of the CM082 (30 mg/kg) group and the corresponding dose of the vehicle group. (a, n = 3) The result of immunohistochemical stain with p-VEGFR-2 in the vehicle-treated group at 7, 14 and 21, days after laser photocoagulated. There are large numbers of yellow granules distributed in vessels, outer plexiform layer, and RPE layer. (b, n = 3) The expression of p-VEGFR-2 in each structure in the CM082-treated group was significantly lower than the control group at the same time point. Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques: Immunohistochemical staining, Staining, Expressing, Control

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Representative CNV lesions in RPE-choroid-sclera flat mounts by perfusion of fluorescein isothiocyanate-dextrcan were obtained 7, 14, and 21 days after photocoagulation. (a, b) The areas of CNV lesions in the vehicle-treated and CM082 group at day 7 were shown and without statistical difference. CM082 (or vehicle) was delivered orally from day 7 ( n = 3). The area of CNV lesions was significantly reduced under CM082 treatment at day 14 (c, d; n = 3) and 21 (e, f; n = 3). (h, i) There is a significantly inhibition of CNV area in CM082 group compared with that in vehicle-treated group ( ∗∗ p < 0.01, ∗∗∗ p < 0.001). (j) The CNV area in the CM082 group showed a regression at day 14 and 21 compared with that in day 7 ( ∗ p < 0.05). Scale bar, 100 μ m.

Article Snippet: Tyrogenex has completed a phase 1 clinical trial of CM082 and is conducting a phase 2b study in patients with exudative AMD.

Techniques: Inhibition

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology and FFA results of CNV modeling. (a) Histology of CNV lesions stained with HE shows that CNV formation and broke the Brunch's membrane at 21 days after photocoagulation. Dome-like CNV complexes, consisting of fibrovascular tissue, retinal pigment epithelial cells, and pigment clumps, are shown and white arrow indicates the vessel lumina of neovascular. (b) FFA results showed fluorescein leakage of CNV in each group at day 14, 21, and 28 (7 days after CM082 treatment) separately. The signal intensity of capillary in background region was defined as “0” whereas the signal intensity of the main branch of the retinal vein was defined as “1”. (c) There is no significant difference between the intensity score of leakage in each group at day 14, 21, and 28 ( p > 0.05). Scale bar, 100 μ m.

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques: Staining, Membrane

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Distribution of CM082 and its metabolites in plasma and eye tissues. (a, b, and c) The concentrations (ng/ml or ng/g) of CM082, X-297, and X-471 in plasma and ocular tissues ( n = 9). There is no significant difference between the concentration of CM082 in plasma and eyes. The same is true for X-297. However, the concentration of X471 in eyes (OS: 16.68 ± 2.18, OD: 15.82 ± 1.85) is obviously lower than that in plasma (32.04 ± 4.57) ( ∗∗ p < 0.01). (d, e, and f) The concentration of CM082, X-297, and X-471 was detected in different ocular tissues ( n = 9). There is no significant difference in concentration of CM082, X-297, and X-471 between OS and OD.

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques: Clinical Proteomics, Concentration Assay

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: FFA results of the CM082 (10 mg/kg/d) group and the corresponding vehicle-treated group at different time points. (a, b; n = 10) FFA showed that the leakage of fluorescein at laser spots are at nearly same extent in vehicle-treated and CM082 group 7 days after laser injury ( p > 0.05, n = 9). (c, d) Leakage of fluorescein in the CM082-treated group was reduced at 21 days after laser injury ( ∗∗ p < 0.01, n = 9).

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques:

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology examine stained with HE of the CM082 (10 mg/kg/d) group ( n = 2) and the corresponding vehicle group ( n = 2) was obtained after FFA examination at day 7, 14, and 21. (a, b) Results showed a smaller CNV size of the CM082-treated group at day14 and 21. CNV complexes consist of retinal pigment epithelial cells, pigment clumps, and vascular tufts were observed. The CNV under CM082 treated was thinner in the center compared with that in the vehicle-treated group. Scale bar, 100 μ m.

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques: Staining

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: FFA results of the CM082 (30 mg/kg/d)-treated group and the corresponding dose of the vehicle-treated group at different time points. Results of FFA showed the leakage of fluorescein at laser spots in vehicle-treated and CM082 group 7 (a, b; n = 10), 14 (c, d; n = 9), and 21 (e, f; n = 8) days after laser injury. (g, h, and i) The fluorescence signal intensity of CM082-treated group was statistically lower than the vehicle-treated group at 14 days and 21 days ( ∗∗∗ p < 0.001). (j) The signal intensity at 14 and 21 days was obviously lower than that at 7 days in the CM082 group ( ∗∗∗ p < 0.001).

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques: Fluorescence

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Histology of CNV lesions stained with hematoxylin-eosin of the CM082 (30 mg/kg) group ( n = 6) and the corresponding dose of the vehicle group ( n = 6) was obtained after FFA examination. Results showed that administration of CM082 reduces laser-induced CNV lesions. (a) In the vehicle-treated group, CNV formed and broke the Brunch's membrane. The depigmentation in RPE, aggregation of macrophage, and neovascularization were obtained 14 days and 21 days after photocoagulation. (b) In the CM082 group, the edema, depigmentation, and CNV areas significantly decreased comparing to vehicle-treated group at the same time point. Scale bar, 100 μ m.

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques: Staining, Membrane

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Immunohistochemical analysis of the CM082 (30 mg/kg) group and the corresponding dose of the vehicle group. (a, n = 3) The result of immunohistochemical stain with p-VEGFR-2 in the vehicle-treated group at 7, 14 and 21, days after laser photocoagulated. There are large numbers of yellow granules distributed in vessels, outer plexiform layer, and RPE layer. (b, n = 3) The expression of p-VEGFR-2 in each structure in the CM082-treated group was significantly lower than the control group at the same time point. Scale bar, 100 μ m.

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques: Immunohistochemical staining, Staining, Expressing, Control

Journal: Journal of Ophthalmology

Article Title: The Effect of CM082, an Oral Tyrosine Kinase Inhibitor, on Experimental Choroidal Neovascularization in Rats

doi: 10.1155/2017/6145651

Figure Lengend Snippet: Representative CNV lesions in RPE-choroid-sclera flat mounts by perfusion of fluorescein isothiocyanate-dextrcan were obtained 7, 14, and 21 days after photocoagulation. (a, b) The areas of CNV lesions in the vehicle-treated and CM082 group at day 7 were shown and without statistical difference. CM082 (or vehicle) was delivered orally from day 7 ( n = 3). The area of CNV lesions was significantly reduced under CM082 treatment at day 14 (c, d; n = 3) and 21 (e, f; n = 3). (h, i) There is a significantly inhibition of CNV area in CM082 group compared with that in vehicle-treated group ( ∗∗ p < 0.01, ∗∗∗ p < 0.001). (j) The CNV area in the CM082 group showed a regression at day 14 and 21 compared with that in day 7 ( ∗ p < 0.05). Scale bar, 100 μ m.

Article Snippet: CM082 is a multitarget tyrosine kinase inhibitor that can suppress neovascularization by inhibiting the VEGF, PDGF, c-kit, and Flt-3 receptor tyrosine kinases.

Techniques: Inhibition