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• 产品描述： PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity

• 靶点： Ki: 4 nM IC50: 9 nM (c-Met);Apoptosis;VEGFR;FGFR;c-Met/HGFR;Bcr-Abl;Autophagy

• 体内研究：
  PHA-665752 (7.5-30 mg/kg/day; i.v. ; for 9 days) exhibits statistically significant dose-dependent tumor growth inhibition of 68%, 39%, and 20% of vehicle control at the 30 mg/kg/day, 15 mg/kg/day, and 7.5 mg/kg/day doses, respectively. PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model.

• 参考文献：
  1. Christensen JG, et al. A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res. 2003 Nov 1;63(21):7345-55. 2. Ma PC. et al. A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin. Clin Cancer Res. 2005 Mar 15;11(6):2312-9.

• 溶解性： DMSO  :  25  mg/mL  (38.96  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.559 ml	7.793 ml	15.586 ml
  5 mM	0.312 ml	1.559 ml	3.117 ml
  10 mM	0.156 ml	0.779 ml	1.559 ml
  50 mM	0.031 ml	0.156 ml	0.312 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 *