Name: LY2801653
Price: 300.00 USD

- Overview
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    Background
    
    LY2801653 is a potent and orally bioavailable inhibitor of c-MET kinase with IC50 value of 2 nM [1].
    C-MET kinase is also known as hepacyte growth factor receptor (HGFR), which is a membrane-associated tyrosine kinase receptor. HGF is the only ligand for this receptor. The binding of HGF induces conformational changes of c-MET and thus activate tyrosine kinase activity, to process downstream signaling. C-MET signaling regulate various cellular functions including cell proliferation, survival and apoptosis, and abnormal activation of c-MET kinase may trigger tumor growth, angiogenesis and metastasis.
    Biochemical study and crystallization study identified LY2801653 was a potent ATP-competitive inhibitor of c-MET kinase, where the inhibition was completed by suppression of c-MET kinase phosphorylation [1]. In vitro study showed that 0.01-10 μM LY2801653 was able to completely block HGF-induced DU-145 cell scattering regulated by c-MET kinase, which demonstrated the inhibition of c-MET kinase activity. When LY2801653 was screened with a panel of cell lines, it was found more potent anti-proliferative activity of LY2801653 in those cell lines with MET gene expression than without MET gene expression [2].
    Mice bearing U-87MG xenograft were treated with low dose (1.3 mg/kg) and high dose (12 mg/kg) LY2801653 once daily for 28 days, and the tissues were characterized. It was found that low dose treatment resulted in a trend of reducing the area of c-MET kinase-associated apoptosis while the high dose treatment resulted in significant reduced apoptosis area. Additionally, high dose resulted in the suppression of c-MET kinase-associated angiogenesis, and vessels tend to be normalized [2].These observations demonstrated the LY2801653 was able to disrupt c-MET kinase downstream signaling via inhibiting the c-MET kinase activity.
    
    [1] Yan S B et al. , LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs. 2012, 31: 833-844.
- Properties
  - Alternative Name
    
    LY-2801653;LY 2801653; N-[3-fluoro-4-[1-methyl-6-(1H-pyrazol-4-yl)indazol-5-yl]oxyphenyl]-1-(4-fluorophenyl)-6-methyl-2-oxopyridine-3-carboxamide
    
    CAS Number
    
    1206799-15-6
    
    Molecular Formula
    
    C30H22F2N6O3
    
    Molecular Weight
    
    552.53
    
    Appearance
    
    A solid
    
    Purity
    
    99.87%
    
    Solubility
    
    ≥27.65 mg/mL in DMSO; insoluble in H2O; ≥5.02 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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