他拉唑帕尼甲苯磺酸盐
| CAS号 | 1373431-65-2 | 货号 | BCP29084 |
| 中文名 | 他拉唑帕尼甲苯磺酸盐 | ||
| 英文名 | Talazoparib tosylate | ||
| 中文别名 | |||
| 英文别名 | BMN 673ts;BMN-673ts;BMN673ts;BMN673; BMN673; BMN-673; LT673; LT 673; LT-673; MDV-3800; MDV 3800; MDV3800; | ||
| 分子式 | C26H22F2N6O4S | 分子量 | 552.55 |
| 生物活性 | Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 nmol/L). Talazoparib acts as an inhibitor of poly ADP ribose polymerase(PARP) which aids in single strand DNA repair. Cells that have BRCA1/2 mutations are susceptible to the cytotoxic effects of PARP inhibitors because of an accumulation of DNA damage. Talazoparib is theorized to have a higher potency than olaparib due to the additional mechanism of action called PARP trapping. PARP trapping is the mechanism of action where the PARP molecule is trapped on the DNA, which interferes with the cells ability to replicate. Talazoparib is found to be ~100 fold more efficient in PARP trapping than olaparib. | ||
| 信号通路 | Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | PARP | ||
结构式
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