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• 产品描述： NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

• 靶点： PI3Kα:2 nM (IC50);PI3Kβ:9.4 nM (IC50);PI3Kδ:14 nM (IC50);PI3Kγ:2.7 nM (IC50);mTOR:5.4 nM (IC50);PI3K; mTOR

• 体外研究：
  NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines

• 体内研究：
  In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight

• 参考文献：
  1. Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.593 ml	7.966 ml	15.932 ml
  5 mM	0.319 ml	1.593 ml	3.186 ml
  10 mM	0.159 ml	0.797 ml	1.593 ml
  50 mM	0.032 ml	0.159 ml	0.319 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 *