JNJ-38158471,951151-97-6

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JNJ-38158471

CAS No. : 951151-97-6

MCE 国际站：JNJ-38158471

产品活性：JNJ-38158471 是一种耐受良好，有口服活性的高选择性 VEGFR-2 抑制剂，IC₅₀ 值为 40 nM。JNJ-38158471 还抑制 Ret 和 Kit ，IC₅₀ 值分别为 180 和 500 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR  |  RET  |  c-Kit

In Vitro: JNJ-38158471 (1-500 nM; 1 hour) inhibits VEGF-stimulated VEGFR-2 autophosphorylation in HUVECs.
JNJ-38158471 (50-1000 nM; 12-16 hours) significantly inhibits VEGF-dependent HUVEC migration. Cellular toxicity is not observed following JNJ-38158471 treatment of HUVECs.

In Vivo: 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 significant activity compare with vehicle treat animals. The body weights of both JNJ-38158471-treated and vehicle-treated groups were comparable at study end.

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