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Gefitinib

Tyrosine kinase inhibitor; Inhibits EGFR

STEMCELL Technologies Inc.

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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.).

CANCER RESEARCH

  • 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.).

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