Name: GSK2636771
Price: 244.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GSK2636771 is a p110β isoform-specific inhibitor of PIK3 with SF50 more than 1 μM [1].PI3K (phosphatidylinositol 3-kinase) has 4 catalytic subunits: p110α, β, δ, γ，and δ. PI3K /AKT and related pathways play important roles in cellular growth and survival via internalizing the effects of external growth factors and membrane tyrosine kinases. [2, 3]. Many studies have shown that PI3K is over activated in a variety of cancer cells and inhibition of this pathway have been focused for cancer patients [4].GSK2636771 is a selective PI3K inhibitor with targeting p110βand has different with the reported GDC-0941 which inhibits all class I PI3K isoforms. In breast cancer cell lines, treatment with GSK2636771 could significantly decrease the phosphorylation of AKT thus inhibits the cell viability. For EEC cell lines with PTEN-mutant, p110β inhibitor GSK2636771 should only combine with p110α selective inhibitor A66 to decrease cell viability [1].
    
    1.Weigelt, B., et al., PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res, 2013. 19(13): p. 3533-44.
    2.Costa, C., et al., Measurement of PIP Levels Reveals an Unexpected Role for p110beta in Early Adaptive Responses to p110alpha-Specific Inhibitors in Luminal Breast Cancer. Cancer Cell, 2014. 24(14): p. 00458-9.
    3.Schwartz, S., et al., Feedback Suppression of PI3Kalpha Signaling in PTEN-Mutated Tumors Is Relieved by Selective Inhibition of PI3Kbeta. Cancer Cell, 2014. 24(14): p. 00459-0.
    4.Slomovitz, B.M. and R.L. Coleman, The PI3K/AKT/mTOR pathway as a therapeutic target in endometrial cancer. Clin Cancer Res, 2012. 18(21): p. 5856-64.
- Properties
  - Alternative Name
    
    2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-morpholin-4-ylbenzimidazole-4-carboxylic acid
    
    CAS Number
    
    1372540-25-4
    
    Molecular Formula
    
    C22H22F3N3O3
    
    Molecular Weight
    
    433.42
    
    Appearance
    
    A solid
    
    Purity
    
    99.78%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥10.83 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

GSK2636771

GSK2636771

Background

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