| 应用 |
A microtubule depolymerizing molecule. |
| 产品介绍 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium是Combretastatin A4 (CA4)的水溶性前体药物，靶向作用于微管，与β-微管蛋白结合， Kd为0.4 μM，可使微管蛋白解聚，IC50为2.4 μM，也干扰肿瘤血管。Phase 3 |
| 备注 |
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds at β-tubulin with Kd of 0.4 μM, inhibits the polymerization of |
| 生化机理 |
Combretastatin A4 Phosphate Disodium Salt is the salt form of Combretastatin A4, a phosphorylated microtubule depolymerizing molecule which induces tumor necrosis by regression of unstable nascent tumor neo-vessels. Studies suggest that Combretastatin A4 Phosphate Disodium Salt selectively inhibits endothelial tumor cells via disrupting VE-cadherin (vascular endothelial-cadherin). In addition, Combretastatin A4 Phosphate Disodium Salt can increase the permeability of endothelial cells while inhibiting their migration and suppress capillary tube formation via disruption of VE-cadherin. Furthermore, Combretastatin A4 Phosphate Disodium Salt can change the morphology of endothelial cells by altering their tubulin cytoskeleton. |
| 别名 |
考布他丁 A-4 磷酸二钠盐; 2-甲氧基-5-[(1Z)-2-(3,4,5-三甲氧基苯基)乙烯基]苯酚磷酸酯二钠盐;CA 4DP; CA 4P;Fosbretabulin disodium salt;Combretastatin A4 disodium phosphate;Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium ;2-Methoxy-5-[(1Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol dihydrogen phosphate disodium salt |
