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• 产品描述： WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.

• 靶点： mTORC1;mTORC2;mTOR:0.19 nM (IC50);PI3Kα:1.179 μM (IC50);PI3Kδ:2.38 μM (IC50);hSMG1:1.25 μM (IC50)

• 体内研究： A single i.v. administration of 50 mg/kg WYE-132 (WYE-125132) into tumor-bearing mice leads to suppression of P-S6K(T389) and P-AKT(S473) for at least 8 hours in PC3MM2, MDA361, HCT116, and HT29 tumors, whereas the steady-state level of P-AKT(T308) is not significantly reduced, indicating that the antitumor efficacy of WYE-132 under such dosing regimens reflects the suppression of mTOR rather than PI3K. Oral administration of WYE-132 causes dose-dependent tumor growth delay in the PI3K/mTOR- and HER2-hyperactive MDA361 tumors with significant antitumor activity at 5 mg/kg, which correlates with a suppression P-S6 and P-AKT(S473) but not P-AKT(T308). An optimal dose of 50 mg/kg WYE-132 induces a substantial regression of large MDA361 tumors. WYE-132 also causes a potent and substantial tumor growth delay in the PTEN-null U87MG glioma

• 参考文献：
  1. Yu K, et al. Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.Cancer Res. 2010 Jan 15;70(2):621-631.

• 溶解性： DMSO  :  25  mg/mL  (48.11  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.925 ml	9.623 ml	19.245 ml
  5 mM	0.385 ml	1.925 ml	3.849 ml
  10 mM	0.192 ml	0.962 ml	1.925 ml
  50 mM	0.038 ml	0.192 ml	0.385 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 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *