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• 产品描述： A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.

• 靶点： p110α:32 nM (IC50);p110α E545K:30 nM (IC50);p110α H1047R:43 nM (IC50);p110γ:3480 nM (IC50);PI3K-C2β:462 nM (IC50);PI4Kβ:236 nM (IC50)

• 体内研究： The optimal dosing strategy for xenograft studies is determined by investigating the drug pharmacokinetics after a dose of 10 mg/kg of body weight by intraperitoneal injection in CD-1 mice. Despite a short half-life of only 0.42 h, the large Cmax (8247 nM) of A66 S that is reached 30 min after dosing ensured that the AUC0-inf (area under the curve from zero time to infinity) (6809 nM•h) is similar to that of BEZ-235 (7333 nM•h), which has a longer half-life of 2.73 h. Furthermore, the A66 on SK-OV-3 tumour tissue is tested using a single dose of 100 mg/kg of body weight to determine whether a long-lasting effect of the drug could be achieved on target tissues. These studies show that A66 causes a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK (extracellular-signal-regulated kinase), at both 1 and 6 h after dosing. Levels of A66 in plasma are determined to be 21.1±1.2 μM and 9.1±1.1 μM at 1 and 6 h after drug injection, whereas levels of A66 in the tumor are 22.7±2.1 μM and 16.0±1.3 μM at the same time points

• 参考文献：
  1. Jamieson S, et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J, 2011, 438(1), 53-62. 2. Sun M, et al. Cancer-derived mutations in the regulatory subunit p85alpha of phosphoinositide 3-kinase function through the catalytic subunit p110alpha. Proc Natl Acad Sci U S A, 2010, 107(35), 15547-15552.

• 溶解度： DMSO  :  50  mg/mL  (127.06  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.541 ml	12.706 ml	25.411 ml
  5 mM	0.508 ml	2.541 ml	5.082 ml
  10 mM	0.254 ml	1.271 ml	2.541 ml
  50 mM	0.051 ml	0.254 ml	0.508 ml

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