Name: AZ5104
Price: 188.00 USD

- Overview
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    Background
    
    AZ5104, is the demethylated metabolite of AZD-9291,is a potent EGFR inhibitor. IC50 <1 nM, 6 nM, 1 nM, 25 nM, for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively.
    EGFR (epidermal growth factor receptor) is a receptor tyrosine kinase on the cell surface. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.
    Compare to AZD9291, AZ5104 has somewhat more potency in mutant EGFR cell lines ex19del (2 nmol/L in PC-9), T790M (2 nmol/L in H1975), and wild-type EGFR (33 nmol/L in LOVO) cell lines. In a phenotypic assay, AZ5104 showed a greater potency across cell lines in a phenotypic assay.
    3 hours after oral dosing in the mouse, the circulating active metabolites in plasma is 33% for AZ5104. In both C/L858R and C/L+T mice, 5 mg/kg/day dose of AZ5104, also show efficacy in shrinking tumors.
- Properties
  - Alternative Name
    
    (Z)-N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylimidic acid
    
    CAS Number
    
    1421373-98-9
    
    Molecular Formula
    
    C27H31N7O2
    
    Molecular Weight
    
    485.58
    
    Appearance
    
    A solid
    
    Purity
    
    99.92%
    
    Solubility
    
    insoluble in H2O; ≥16.95 mg/mL in DMSO; ≥5.86 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

AZ5104

AZ5104

Background

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