Gefitinib

- Overview
  - Gefitinib is commonly used as an anti-lung and anti-breast cancer agent. Gefitinib acts as an inhibitor of mutated or overactive epidermal growth factor receptor (EGFR) by binding to the ATP binding site. Because epidermal growth factors are responsible for controlling cell growth and proliferation, a mutated form would likely facilitate cancer growth and development. Gefitinib is sparingly soluble in aqueous solution (0.027 mg/mL).
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    Background
    
    Gefitinib is a selective inhibitor of epidermal growth factor receptor's tyrosine kinease domain. Gefitinib inhibits EGFR tyrosine kinase by binding to the adenosine triphosphate (ATP)-binding site of the enzyme.
- Properties
  - CAS Number
    
    184475-35-2
    
    Molecular Formula
    
    C22H24CIFN4O3
    
    Molecular Weight
    
    446.902
    
    Appearance
    
    White or off-white powder
    
    Other Properties
    
    Source: Synthetic
    Water Content (Karl Fischer): ≤0.2%
    Assay: (On Dried Basis): 98.0-101.0%
    Melting Point: 198-203°C
    
    Storage
    
    -20 °C
    
    * For research use only
- Applications
  - Application Description
    
    Cancer Applications: EGFR is overexpressed in the cells of certain types of human carcinomas. This leads to inappropriate activation of the anti-apoptotic Ras signalling cascade, eventually leading to uncontrolled cell proliferation.