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• 产品描述： AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.

• 靶点： PI3Kα:935 nM (IC50);PI3Kγ:30 nM (IC50);PI3Kδ:20 μM (IC50);PI3Kβ:20 μM (IC50);CaseinKinase; PI3K

• 体内研究：
  Oral administration of AS-252424 in a mouse model of acute peritonitis leads to a significant reduction of leukocyte recruitment. To evaluate the efficacy of AS-252424 to block leukocyte migration in vivo, it is tested in a mouse model of thioglycollate-induced peritonitis. Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%±14%), almost matching the result observed in PI3Kγ-deficient mice. Given the short oral half-life of AS-252424 (t1/2=1 h) and relative high clearance (2.25 L/kg per h), investigations at later time points (24-48 h) to assess macrophage and monoycyte recruitment are not undertaken. The modest pharmacokinetic properties do not appear to be caused by rapid oxidative metabolism (microsomal metabolism after 1 h: 16% (rat), 10% (human))

• 参考文献：
  1. Pomel V, et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J Med Chem. 2006 Jun 29;49(13):3857-71.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.276 ml	16.378 ml	32.757 ml
  5 mM	0.655 ml	3.276 ml	6.551 ml
  10 mM	0.328 ml	1.638 ml	3.276 ml
  50 mM	0.066 ml	0.328 ml	0.655 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 *