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• 产品描述： GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.

• 靶点： Aurora B:0.38 nM (Ki);Aurora C:1.5 nM (Ki);Apoptosis; Tie-2; FLT; AMPK; AuroraKinase

• 体内研究：
  In nude mice implanted with human colon tumor (HCT116) xenografts, a single dose of GSK-1070916 administered i.p. inhibits HH3-S10 phosphorylation in a dose-dependent manner. Repeated i.p. administration of GSK-1070916 produces complete or partial antitumor activity in 4 of 8 tumor types [lung, A549; colon, HCT116; acute myelogenous leukemia (AML), HL60; and chronic myelogenous leukemia, K562], stable disease in 3 of 8 (colon, Colo205; lung, H460; and breast, MCF-7), and tumor growth delay in 1 of 8 tumor types (colon, SW620). Daily administration of GSK-1070916 is generally well-tolerated

• 参考文献：
  1. Adams ND, et al. Discovery of GSK-1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001. 2. Hardwicke MA, et al. GSK-1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models. Mol Cancer Ther. 2009 Jul;8(7):1808-17.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.97 ml	9.85 ml	19.699 ml
  5 mM	0.394 ml	1.97 ml	3.94 ml
  10 mM	0.197 ml	0.985 ml	1.97 ml
  50 mM	0.039 ml	0.197 ml	0.394 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 *