PD 153035 is a potent, reversible inhibitor of EGFR kinase (Ki = 5.2 pM; IC50 = 29 pM).1 It less effectively inhibits HER2 (IC50 = 2.3 µM) and has little effect on several other receptor and non-receptor tyrosine kinases.1 PD 153035 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.2,3
1.Fry, D.W., Kraker, A.J., McMichael, A., et al.A specific inhibitor of the epidermal growth factor receptor tyrosine kinaseScience265(5175)1093-1095(1994) 2.Bos, M., Mendelsohn, J., Kim, Y.M., et al.PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent mannerClinical Cancer Research3(11)2099-2106(1997) 3.Rae, J.M., and Lippman, M.E.Evaluation of novel epidermal growth factor receptor tyrosine kinase inhibitorsBreast Cancer Research and Treatment83(2)99-107(2004)