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• 产品描述： AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.

• 靶点： IC50: 880 nM (RET), 170 nM (KDR), 790 nM (Flt-4), 500 nM (c-Kit), 520 nM (Flt-3), 20 nM (Abl);VEGFR;FLT;c-RET;Bcr-Abl;c-Kit

• 体内研究：
  After a single oral administration of 15 mg/kg of AST 487 to OF1 mice, a mean peak plasma level (Cmax) of 0.505±0.078 μM SE is achieved after 0.5 h. Similar levels of AST 487 are found in the plasma of mice up to 6 h after oral administration, with a Clast of 21±4 nM at 24 h. The oral bioavailability is calculated to be 9.7% with a t1/2 terminal elimination of 1.5 h

• 参考文献：
  1. Akeno-Stuart N, et al. The RET Kinase Inhibitor NVP-AST487 Blocks Growth and Calcitonin Gene Expression through Distinct Mechanisms in Medullary Thyroid Cancer Cells. Cancer Res. 2007 Jul 15;67(14):6956-64. 2. Weisberg E, et al. Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells. Blood. 2008 Dec 15;112(13):5161-70.

• 溶解性： Soluble  in  DMSO

• 保存条件： −20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.888 ml	9.442 ml	18.884 ml
  5 mM	0.378 ml	1.888 ml	3.777 ml
  10 mM	0.189 ml	0.944 ml	1.888 ml
  50 mM	0.038 ml	0.189 ml	0.378 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 *