产品
编 号：F535835
分子式：C15H17ClN6O3
分子量：364.79
分子式：C15H17ClN6O3
分子量：364.79
产品类型
规格
价格
是否有货
1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 951151-97-6
产品详情
生物活性：
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
体内研究：
JNJ-38158471 (10 or 100 mg/kg; p.o.; once-daily) inhibits VEGF-induced corneal neovascularization.JNJ-38158471 (10-200 mg/kg; p.o.) inhibits the growth of human tumor xenografts in a dose-dependent manner in both A431 and HCT116 models. JNJ-38158471 treatment is well tolerated, following continuous administration for 24 days, body weights were comparable with control animals.JNJ-38158471 (100 mg/kg; p.o.; once-daily) treatment shows statistically signi?cant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end.Animal Model:Female C57BL/6J mice are implanted with rhVEGF165
Dosage:10 or 100 mg/kg
Administration:Daily oral administration for 6 days
Result:Caused a marked and apparently dose-dependent inhibition of VEGF-dependent blood vessel formation (100 mg/kg, resulted in 83% inhibition; 10 mg/kg, resulted in 15% inhibition).
Animal Model:Female athymic nude mice; 5-6 weeks; implanted subcutaneously human colorectal carcinoma cells (HCT116) or human epidermoid carcinoma cells (A431)
Dosage:10, 50, 100, 200 mg/kg
Administration:Oral administration for 35 days
Result:Achieved optimum ef?cacy with the dose from 100 to 200 mg/kg daily.
Animal Model:Female athymic nude mice; 5-6 weeks; implanted subcutaneously human skin melanoma cells (A375)
Dosage:100 mg/kg
Administration:Once-daily oral administration for 28 days
Result:Inhibited 90% growth of tumor with daily doses of 100 mg/kg.
Animal Model:Female C57BL/6J-Apc Min mice; 5 weeks of age
Dosage:100 mg/kg
Administration:Once-daily oral administration for two weeks
Result:Inhibited polyp formation in the transgenic APC min-mouse model.
体外研究：
JNJ-38158471 (1-500 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 autophosphorylation in HUVECs.JNJ-38158471 (50-1000 nM; 12-16 hours) signi?cantly inhibits VEGF-dependent HUVEC migration. Cellular toxicity is not observed following JNJ-38158471 treatment of HUVECs.
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
体内研究：
JNJ-38158471 (10 or 100 mg/kg; p.o.; once-daily) inhibits VEGF-induced corneal neovascularization.JNJ-38158471 (10-200 mg/kg; p.o.) inhibits the growth of human tumor xenografts in a dose-dependent manner in both A431 and HCT116 models. JNJ-38158471 treatment is well tolerated, following continuous administration for 24 days, body weights were comparable with control animals.JNJ-38158471 (100 mg/kg; p.o.; once-daily) treatment shows statistically signi?cant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end.Animal Model:Female C57BL/6J mice are implanted with rhVEGF165
Dosage:10 or 100 mg/kg
Administration:Daily oral administration for 6 days
Result:Caused a marked and apparently dose-dependent inhibition of VEGF-dependent blood vessel formation (100 mg/kg, resulted in 83% inhibition; 10 mg/kg, resulted in 15% inhibition).
Animal Model:Female athymic nude mice; 5-6 weeks; implanted subcutaneously human colorectal carcinoma cells (HCT116) or human epidermoid carcinoma cells (A431)
Dosage:10, 50, 100, 200 mg/kg
Administration:Oral administration for 35 days
Result:Achieved optimum ef?cacy with the dose from 100 to 200 mg/kg daily.
Animal Model:Female athymic nude mice; 5-6 weeks; implanted subcutaneously human skin melanoma cells (A375)
Dosage:100 mg/kg
Administration:Once-daily oral administration for 28 days
Result:Inhibited 90% growth of tumor with daily doses of 100 mg/kg.
Animal Model:Female C57BL/6J-Apc Min mice; 5 weeks of age
Dosage:100 mg/kg
Administration:Once-daily oral administration for two weeks
Result:Inhibited polyp formation in the transgenic APC min-mouse model.
体外研究：
JNJ-38158471 (1-500 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 autophosphorylation in HUVECs.JNJ-38158471 (50-1000 nM; 12-16 hours) signi?cantly inhibits VEGF-dependent HUVEC migration. Cellular toxicity is not observed following JNJ-38158471 treatment of HUVECs.
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