S87891 |
JNJ-38158471 |
源叶(MedMol) | 98% |
- 产品描述: 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
- 靶点: VEGFR-2:40 nM (IC50);RET:180 nM (IC50);c-Kit:500 nM (IC50);VEGFR; c-RET; c-Kit
- 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 significant 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).
- 参考文献:
1. Kenneth RL, et, al. A Highly Selective, Orally Bioavailable, Vascular Endothelial Growth Factor receptor-2 Tyrosine Kinase Inhibitor Has Potent Activity in Vitro and in Vivo. Angiogenesis. 2009; 12(3): 287-96.
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.741 ml 13.707 ml 27.413 ml 5 mM 0.548 ml 2.741 ml 5.483 ml 10 mM 0.274 ml 1.371 ml 2.741 ml 50 mM 0.055 ml 0.274 ml 0.548 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)