奥瑞布林
| CAS号 | 181816-48-8 | 货号 | BCP07754 |
| 中文名 | 奥瑞布林 | ||
| 英文名 | Ombrabulin | ||
| 中文别名 | |||
| 英文别名 | AVE-8062; AVE 8062; AVE8062; | ||
| 分子式 | C21H26N2O6 | 分子量 | 402.44 |
| 生物活性 | Ombrabulin is a synthetic water-soluble analogue of combretastatin A4, derived from the South African willow bush (Combretum caffrum), with potential vascular-disrupting and antineoplastic activities. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrata, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis. Ombrabulin was discovered by Ajinomoto and under development by Sanofi-Aventis. It is currently in Phase III clinical trials for the treatment of advanced-stage soft-tissue sarcoma. Ombrabulin was granted orphan drug status by the European Medicines Agency in April 2011. Ombrabulin is a combretastatin A-4 derivative that exerts its antitumor effect by disrupting the formation of blood vessels needed for tumor growth. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage | ||
| 靶 点 | Microtubule VDA | ||
结构式
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