Name: INK1117
Price: 329.00 USD

- Overview
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    Background
    
    IC50: 15nM: inhibits phosphoinositide 3-kinase α (PI3Kα) in vitro.INK1117 is a novel, potent and selective inhibitor of PI3Kα with potential antineoplastic activity, which may induce tumor cell apoptosis and growth inhibition in PI3Kα-expressing tumor cells. INK1117 dampens signaling to Akt and suppresses the growth of cancer cells harboring wild-type or mutated p110α. PI3Ks, a family of eight lipid kinase enzymes, produce 3-phosphorylated phosphoinositides in cellular membranes and are promising targets for therapeutic development in cancer.In vitro: INK1117 blocked class I PI3K enzymes (p110α, p110β, p110γ or p110δ) in the low to mid-nanomolar range in human natural killer (NK) cell lines. INK1117 selectively inhibited PI3K signaling in cellular assays when used at 0.1-1 μM. INK1117 selectively dampened p110 α when used at 1 μM. INK1117 did not inhibit production of IFN-γ protein in cells with anti-NKG2D, indicating that INK1117 did not decrease IFN-γ mRNA [1].In vivo: Female C57BL/6 mice were orally given INK1117 at a dose of 60 mg/kg using a sterile disposable 20G-1.5” feeding needle. After 8 days, INK1117 had negligible effects on NK cell maturation or survival. However, INK1117 did not show significantly decrease in the percentage of B cells and did not alter the percentages of T cells or the fractions of CD4 and CD8 T cells, the percentages of NK cells in bone marrow and spleen [1].
- Properties
  - Alternative Name
    
    MLN1117,TAK-117; [6-(2-amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinyl-methanone
    
    CAS Number
    
    1268454-23-4
    
    Molecular Formula
    
    C19H17N5O3
    
    Molecular Weight
    
    363.4
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤1mg/ml in DMSO;0.25mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

INK1117

INK1117

Background

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