瓦他拉尼碱
| 中文名称 | 瓦他拉尼碱 |
|---|---|
| 中文同义词 | 瓦特拉尼碱;伐他拉尼;N-(4-氯苯基)-4-(吡啶-4-基甲基)二氮杂萘-1-胺;瓦他拉尼碱;瓦他拉尼碱双盐酸盐;N-(4-氯苯基)-4-(吡啶-4-基甲基)酞嗪-1-胺;伐拉尼布;二盐酸瓦他拉尼(VEGFR抑制剂) |
| 英文名称 | Vatalanib base |
| 英文同义词 | N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine;N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)- 1-Phthalazinamine;1-PhthalazinaMine, N-(4-chlorophenyl)-4-(4-pyridinylMethyl)-;Vatalanib (PTK787) Dihydrochloride Base;Pynasunate, ZK222584, CGP-79787, PTK 787;(4-Chloro-phenyl)-(4-pyridin-4-ylmethyl-phthalazin-1-yl)-amine;Vatalanib (free base);VATALANIB |
| CAS号 | 212141-54-3 |
| 分子式 | C20H15ClN4 |
| 分子量 | 346.81 |
| EINECS号 | |
| 相关类别 | Antineoplastic |
| Mol文件 | 212141-54-3.mol |
| 结构式 |  |
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) |
|
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.
安全信息
| 海关编码 | 2933399990 |
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