Gefitinib is a selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase that binds competitively in the ATP binding pocket with IC50 values of 23 and 80 nM for A431 vulval squamous carcinoma cells and KB cells, respectively (Barker et al.)
Blocks proliferation in vitro and in mouse xenograft models, of multiple cancer cell types including colon, ovarian, and breast cancer cell lines (Ciardiello et al.)
Induces apoptosis in the HaCaT human keratinocyte cell line via a c-Jun N-terminal kinase (JNK) activation, an EGFR-independent mechanism (Lu et al.)