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• 产品描述： PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy

• 靶点： p110α:8 nM (IC50);p110β:88 nM (IC50);p110δ:48 nM (IC50);p110γ:150 nM (IC50);mTORC1:20 nM (IC50);mTORC2:83 nM (IC50);PI3KC2β:26 nM (IC50);PI3KC2α:1 μM (IC50);hsVPS34:2.3 μM (IC50);DNA-PK:2 nM (IC50);ATR:850 nM (IC50);ATM:920 nM (IC50);PI4KIIIβ:50 μM (IC50);Apoptosis; DNA-PK; PI3K; mTOR; Autophagy

• 体内研究：
  PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects. PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells

• 参考文献：
  1. Raynaud FI, et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther. 2009 Jul;8(7):1725-39. 2. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110 alpha. Cell. 2006 May 19;125(4):733-47. 3. Park S, et al. PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase anLeukemia. 2008 Sep;22(9):1698-706.d mTOR, has antileukemicactivity in AmL. Leukemia. 2008 Sep;22(9):1698-706. 4. López-Fauqued M, et al. The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of melanoma cells. Int J Cancer. 2010 Apr 1;126(7):1549-61.

• 溶解性： DMSO  :  10  mg/mL  (28.71  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.871 ml	14.353 ml	28.706 ml
  5 mM	0.574 ml	2.871 ml	5.741 ml
  10 mM	0.287 ml	1.435 ml	2.871 ml
  50 mM	0.057 ml	0.287 ml	0.574 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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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 *