瓦他拉尼碱
瓦他拉尼碱 性质
| 熔点 | 209-212° |
|---|---|
| 沸点 | 587.8±50.0 °C(Predicted) |
| 密度 | 1.330±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C(protect from light) |
| 溶解度 | DMSO 中≥16.85 mg/mL； ≥3.0125 mg/mL，乙醇溶液，温和加热和超声波；温和加热和超声波下，水中≥32.53 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 5.46±0.10(Predicted) |
瓦他拉尼碱 用途与合成方法
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VEGFR2 37 nM (IC 50 ) |
Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC 50 of 270 nM, 730 nM and 580 nM, respectively. Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC 50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2.
Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes.
