中文名 | 瓦他拉尼碱 |
英文名 | Vatalanib base |
别名 | 伐他拉尼 瓦特拉尼碱 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 N-(4-氯苯基)-4-(吡啶-4-基甲基)二氮杂萘-1-胺 |
英文别名 | Pynasunate Vatalanib base PTK787 free base Vatalanib free base (PTK787 free base Vatalanib (PTK787) Dihydrochloride Base Pynasunate, ZK222584, CGP-79787, PTK 787 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)- (4-Chloro-phenyl)-(4-pyridin-4-ylmethyl-phthalazin-1-yl)-amine |
CAS | 212141-54-3 |
化学式 | C20H15ClN4 |
分子量 | 346.81 |
InChI | InChI=1/C20H15ClN4/c21-15-5-7-16(8-6-15)23-20-18-4-2-1-3-17(18)19(24-25-20)13-14-9-11-22-12-10-14/h1-12H,13H2,(H,23,25) |
密度 | 1.330±0.06 g/cm3(Predicted) |
熔点 | 209-212° |
沸点 | 587.8±50.0 °C(Predicted) |
闪点 | 309.3°C |
蒸汽压 | 8.48E-14mmHg at 25°C |
折射率 | 1.711 |
酸度系数 | 5.46±0.10(Predicted) |
存储条件 | 2-8°C(protect from light) |
体外研究 | 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. |
体内研究 | 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. |
上游原料 | 1-氯-4-(4-吡啶基甲基)酞嗪 3-羟基-2-(吡啶-4-基)茚-1-酮 苯酞 对氯碘苯 4-氯苯胺 4-溴氯苯 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.883 ml | 14.417 ml | 28.834 ml |
5 mM | 0.577 ml | 2.883 ml | 5.767 ml |
10 mM | 0.288 ml | 1.442 ml | 2.883 ml |
5 mM | 0.058 ml | 0.288 ml | 0.577 ml |
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