Afatinib

- Overview
  - Afatinib is an anilinoquinazoline derivative with a reactive acrylamide group. It is a tyrosine kinase inhibitor and blocks enzymatically active ErbB (proto-oncogene B of the avian erythroblastosis virus AEV-H strain) receptor family members.
    
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    Background
    
    Afatinib is an irreversible ErbB-family blocker. The reactive acrylamide group is important as it differentiates Afatinib from other ErbB targeting agents by inhibiting the activity of the kinases found in all members of the ErbB family.
- Properties
  - CAS Number
    
    850140-72-6
    
    Molecular Formula
    
    C24H25ClFN5O3
    
    Molecular Weight
    
    485.94
    
    Appearance
    
    White to off-white powder
    
    Solubility
    
    DMSO (97 mg/ml), ethanol (15 mg/ml) and water (<1 mg/ml) at 25 °C).
    
    Other Properties
    
    Source: Synthetic
    Purity Level: ≥99% (by HPLC)
    
    Storage
    
    -20°C
    
    * For research use only
- Applications
  - Application Description
    
    Cancer Applications: Deregulation of the ErbB receptor network is a driver in epithelial cancers. Afatinib inhibits ErbB-4 and the proliferation of cancer cell lines driven by multiple ErbB receptor aberrations at concentrations below 100 nM (Solca et al, 2012). Afatinib showed positive results during in vitro assays against a variety of human cancer cell lines, including human epidermoid carcinoma cell line A431, murine NIH-3T3 cells, breast cancer cell line BT-474, and gastric cancer cell line NCI-N87. (Li et al, 2008).