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

• 靶点： PLK1:0.8 nM (IC50);PLK2:16.9 nM (IC50);PLK3:50.2 nM (IC50);FAK/PTK2:19.6 nM (IC50);MLCK/MYLK:25.6 nM (IC50);FES/FPS:58.2 nM (IC50)

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

• 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.

• 溶解性： DMSO  :  16.67  mg/mL  (29.68  mM;  ultrasonic  and  warming  and  heat  to  60°C)

• 保存条件： RT

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.781 ml	8.903 ml	17.806 ml
  5 mM	0.356 ml	1.781 ml	3.561 ml
  10 mM	0.178 ml	0.89 ml	1.781 ml
  50 mM	0.036 ml	0.178 ml	0.356 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *