TAK-960 monohydrochloride

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TAK-960 monohydrochloride 

TAK-960 monohydrochloride 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 monohydrochloride 对 PLK2 和 PLK3 也有抑制作用,IC50 分别为 16.9 和 50.2 nM。TAK-960 monohydrochloride 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。

TAK-960 monohydrochloride

TAK-960 monohydrochloride Chemical Structure

CAS No. : 2108449-45-0

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TAK-960 monohydrochloride 的其他形式现货产品:

TAK-960 TAK-960 dihydrochloride

生物活性

TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts[1].

体外研究
(In Vitro)

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 EC50 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

598.06

Formula

C27H35ClF3N7O3

CAS 号

2108449-45-0

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.

    [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.

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