TAK-960 monohydrochloride T39553

Product Introduction
Bioactivity


英文名: TAK-960 monohydrochloride

描述: TAK-960 monohydrochloride is an orally available compound that selectively inhibits polo-like kinase 1 (PLK1) with an IC 50 of 0.8 nM. It also demonstrates inhibitory activity against PLK2 (IC 50 of 16.9 nM) and PLK3 (IC 50 of 50.2 nM). Moreover, TAK-960 monohydrochloride effectively suppresses the proliferation of various cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.

体外活性: TAK-960 monohydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 monohydrochloride (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC 50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells[1]. TAK-960 monohydrochloride (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.

体内活性: TAK-960 monohydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts[1]. In animal models, TAK-960 monohydrochloride (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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: TAK 960 Monohydrochloride | TAK960 Monohydrochloride | TAK960 monohydrochloride | TAK960 | TAK 960 | TAK-960 Monohydrochloride | TAK 960 monohydrochloride | TAK-960

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途