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• 产品描述： MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.

• 靶点： Aurora A:4 nM (IC50);CaseinKinase; PKA; Src; AuroraKinase

• 体内研究：
  In the HCT-116 tumor-bearing mice, MLN8054 treatment inhibits tumor growth dose dependently. MLN8054 is generally well tolerated. MLN8054 also inhibits the growth of the PC-3 tumor xenograft in nude mice. MLN8054 Treatment Results in Inhibition of Aurora A, Accumulation of Mitotic Cells, and Apoptosis in vivo. MLN8054 selectively inhibits Aurora A kinase activity when dosed at 30 mg/kg. At this dose in HCT116 tumor tissue, MLN8054 has been shown to inhibit Aurora A autophosphorylation, and induce an increase in the Aurora B substrate, pHisH3

• 参考文献：
  1. Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. 2. Huck JJ, et al. MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Mol Cancer Res. 2010 Mar;8(3):373-84.

• 溶解性： DMSO  :  20.83  mg/mL  (43.68  mM;  ultrasonic  and  warming  and  heat  to  60°C)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.097 ml	10.485 ml	20.971 ml
  5 mM	0.419 ml	2.097 ml	4.194 ml
  10 mM	0.21 ml	1.049 ml	2.097 ml
  50 mM	0.042 ml	0.21 ml	0.419 ml

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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 分子摩尔量 (g/mol)

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