瓦他拉尼堿
| 中文名稱 | 瓦他拉尼堿 |
|---|---|
| 中文同義詞 | 瓦特拉尼堿;伐他拉尼;N-(4-氯苯基)-4-(吡啶-4-基甲基)二氮雜萘-1-胺;瓦他拉尼堿;瓦他拉尼堿雙鹽酸鹽;N-(4-氯苯基)-4-(吡啶-4-基甲基)酞嗪-1-胺;伐拉尼布;二鹽酸瓦他拉尼(VEGFR抑制劑) |
| 英文名稱 | Vatalanib base |
| 英文同義詞 | 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);SORAFENIB BASE VATALANIB |
| CAS號 | 212141-54-3 |
| 分子式 | C20H15ClN4 |
| 分子量 | 346.81 |
| EINECS號 | 202-303-5 |
| 相關(guān)類別 | Antineoplastic |
| Mol文件 | 212141-54-3.mol |
| 結(jié)構(gòu)式 |  |
瓦他拉尼堿 性質(zhì)
| 熔點 | 209-212° |
|---|---|
| 沸點 | 587.8±50.0 °C(Predicted) |
| 密度 | 1.330±0.06 g/cm3(Predicted) |
| 儲存條件 | 2-8°C(protect from light) |
| 溶解度 | DMSO 中≥16.85 mg/mL； ≥3.0125 mg/mL，乙醇溶液，溫和加熱和超聲波；溫和加熱和超聲波下，水中≥32.53 mg/mL |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 5.46±0.10(Predicted) |
| 顏色 | 淺黃至黃色 |
|
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
| 海關(guān)編碼 | 2933399990 |
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