TAK-960 hydrochloride是一种有效的，可口

TAK-960 hydrochloride

TAK-960 hydrochloride是一种有效的，可口服的，选择性的 polo-like kinase 1 (PLK1) 抑制剂，IC₅₀ 为 0.8 nM。TAK-960 hydrochloride 对 PLK2 和 PLK3 也有抑制作用，IC₅₀ 分别为 16.9 和 50.2 nM。TAK-960 hydrochloride 抑制多种肿瘤细胞系的增殖，对多种肿瘤异种移植具有显著的疗效。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

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. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts[1].

体外研究(In Vitro)    
TAK-960 hydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 hydrochloride (2-1000 nM; 72 hours) 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[1].
TAK-960 hydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells[2].

Cell Viability Assay[1]

Cell Line:    HT-29, HCT116, COLO320DM, HCT-15, RKO, SW480, K-562….Hela, DU 145 cells
Concentration:    2-1000 nM
Incubation Time:    72 hours
Result:    Inhibited proliferation of human cancer cell lines regardless of TP53 and KRAS mutation and MDR1 expression status.

体内研究(In Vivo)    
TAK-960 hydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts[1].
In animal models, TAK-960 hydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts[1].

Animal Model:    nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)[1]
Dosage:    10 mg/kg
Administration:    P.o.; once daily for 2 weeks
Result:    Substantial antitumor activity and good tolerability.

Formula    
C27H34F3N7O3.ClH

CAS 号    
1137868-96-2

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Please store the product under the recommended conditions in the Certificate of Analysis.
 

参考文献

[1]. Hikichi Y, et al. TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar;11(3):700-9.  [Content Brief] [2]. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.  [Content Brief]