• 产品描述： ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer

• 靶点： PI3Kα：22.0 nM (IC50)；PI3Kδ：39.8 nM (IC50)；PI3Kβ：129.0 nM (IC50)；PI3Kγ：717.3 nM (IC50)；mTOR：152.0 nM (IC50)；DNA-PK：70.6 nM (IC50);DNA-PK;PI3K;mTOR

• 体外研究：
  ETP-45658 (10 μM; 4 h) decreases in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells.
  
  ETP-45658 inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells, with EC50s of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, respectively.
  
  ETP-45658 (10 μM; 24 h) induces a clear G1 arrest of PC3 cells.
  
  ETP-45658 inhibits the mutant PI3Kα proteins, H1047R and E545K, with IC50s of 16.8 nM and 13.1 nM, respectively.
  
  ETP-45658 (5 nM-11.1 μM; 1 h) induces a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells.
  
  ETP-45658 (10 μM; 1 h) decrease the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells.

• 体内研究：
  ETP-45658 (22.7 mg/kg) decreases the level of phosphorylated Akt on serine 473 in the mammary ducts of transgenic mice.

• 参考文献：
  1. Link W, et, al. Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J Biol Chem. 2009 Oct 9;284(41):28392-28400.
  
  2. Hill R, et, al. A novel phosphatidylinositol 3-kinase (PI3K) inhibitor directs a potent FOXO-dependent, p53-independent cell cycle arrest phenotype characterized by the differential induction of a subset of FOXO-regulated genes. Breast Cancer Res. 2014 Dec 9;16(6):482.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 备注： ETP-45658 是一种有效的 PI3K 抑制剂，抑制 PI3Kα，PI3Kδ，PI3Kβ 和 PI3Kγ的 IC50 值分别为 22.0 nM，39.8 nM，129.0 nM 和 717.3 nM。ETP-45658 还可以抑制 DNA-PK (IC50=70.6 nM) 和 mTOR (IC50=152.0 nM)。

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.212 ml	16.06 ml	32.119 ml
  5 mM	0.642 ml	3.212 ml	6.424 ml
  10 mM	0.321 ml	1.606 ml	3.212 ml
  50 mM	0.064 ml	0.321 ml	0.642 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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• pg ng μg mg g kg =
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