Name: PKI-402
Price: 426.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    PKI-402 is a selective, equipotent and ATP-competitive class I PI3K inhibitor (IC50= 1 nM, 7 nM, 16 nM and 14 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.)
    
    PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.
    
    In multiple human cancer cell lines (e.g. breast, brain, pancreas and NSCL), PKI-402 inhibited growth of cancer cells, and attenuated phosphorylation of effector of PI3K and mTOR. In MDA-MB-361, 30 nM PKI-402 caused cleaved of the apoptosis marker—PARP.
    
    In MDA-MB-361 mouse tumor xenograft models, administration of 100 mg/kg of PKI-402 daily for 5 days decreased the initial tumor volume from 260 mm3 to 129 mm3 and inhibited tumor regrowth for 70 days, single dose of PKI-402 blocked phosphorylation of Akt and led to cleaved PARP.
- Properties
  - Alternative Name
    
    1-[4-(3-ethyl-7-morpholin-4-yltriazolo[4,5-d]pyrimidin-5-yl)phenyl]-3-[4-(4-methylpiperazine-1-carbonyl)phenyl]urea
    
    CAS Number
    
    1173204-81-3
    
    Molecular Formula
    
    C29H34N10O3
    
    Molecular Weight
    
    570.65
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥14.28 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

PKI-402

PKI-402

Background

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