Overactivity of the epidermal growth factor receptor-associated tyrosine kinase (EGFR) has been associated with cancer development and progression, including cell proliferation, apoptosis, angiogenesis, and metastatic spread. PD 153035 is a highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC50 = 29 pM). It has been shown to rapidly suppress autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells, as well as to selectively block EGF-mediated cellular processes, including mitogenesis and early gene expression.
