TAK-960 hydrochloride
| CAS号 | 1137868-96-2 | 货号 | BCP28992 |
| 中文名 | TAK-960 hydrochloride | ||
| 英文名 | TAK-960 hydrochloride | ||
| 中文别名 | |||
| 英文别名 | TAK960 hydrochloride; TAK 960 hydrochloride; | ||
| 分子式 | C27H34F3N7O3.HCl | 分子量 | 598.06 |
| 生物活性 | TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. IC50 & Target: IC50: 0.8 nM (PLK1, + ATP), 16.9 nM (PLK2, + ATP), 50.2 nM (PLK3, + ATP)[1] In Vitro: TAK-960 inhibits full-length PLK1 protein with IC50 of 0.8 nM, wich is 20-fold lower than the next lowest IC50 value (PLK2: 16.9 nM). TAK-960 (2-1000 nM) causes accumulation of G2-M cells in HT-29 cells. TAK-960 inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells. TAK-960 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells. TAK-960 does not sensitize cancer cells to radiation when an insufficient amount of time is provided to induce mitotic arrest. The overexpression of a PLK1 mutant, PLK1-R136G&T210D;, which is confirmed to cancel the TAK-960-mediated increase in the proportion of mitotic cells, abrogates the radiosensitizing effects of TAK-960[2]. In Vivo: TAK-960 (7.5 mg/kg, p.o.) shows a significant increase in median survival compared with vehicle in MV4-11 human leukemia model. TAK-960 (10 mg/kg, p.o.) inhibits tumor growth in the MDR1-expressing K562ADR-bearing leukemia xenograft model. TAK-960 (10 mg/kg) significantly suppresses tumor growth when combined with IR in tumor xenografts. | ||
| 信号通路 | Cell Cycle/DNA Damage | ||
| 靶 点 | PLK | ||
结构式
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