TAK-960 hydrochloride

参考资料仅供科学研究，不可用于个人用途。

货号：BCP28992CAS号：1137868-96-2纯度：98%

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基本信息与产品描述

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;
SMILES	O=C1C(F)(F)CN(C3CCCC3)C(N=C(NC4=CC(F)=C(C(NC5CCN(C)CC5)=O)C=C4OC)N=C2)=C2N1C.Cl
化学名称
分子式	C27H34F3N7O3.HCl	分子量	598.06
纯度	98%	配送	惯例下常温包邮
产品描述	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.

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TAK-960 hydrochloride

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