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TAK-960 monohydrochloride

产品编号 T39553 CAS 2108449-45-0

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.

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TAK-960 monohydrochloride Chemical Structure

TAK-960 monohydrochloride, CAS 2108449-45-0

规格	价格/CNY		货期	数量
10 mg	￥ 5,770		35日内发货
50 mg	￥ 24,100		35日内发货

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TAK-960 monohydrochloride 的其他形式现货产品:

TAK-960

其他形式的 TAK-960 monohydrochloride:

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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.

分子量	598.07
分子式	C27H35ClF3N7O3
CAS No.	2108449-45-0

存储

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

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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.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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