183322-45-4

PD153035 is an inhibitor of EGFR, competitive with ATP. EGF Receptor: IC50 = 25 pM (Ki = 6 pM).

ChEBI: A hydrochloride obtained by combining PD-153035 with one equivalent of hydrochloric acid.

PD153035 is apotent and selective ATP competitive inhibitor of the epidermal growth factor receptor tyrosine kinase EGFR.

This extraordinarily potent EGFR inhibitor (F.Wt. = 396.67 (as hydrochloride); CAS 183322-45-4 (hydrochloride), 153436-54-5 (free base); Solubility (25°C) : <1 mg/mL DMSO, <1 mg/mL Water), also known systematically as N- (3-bromophenyl) -6,7-dimethoxyquinazolin-4-amine, rapidly suppresses in vitro EGFR autophosphorylation (Ki = 5.2 pM; IC50 = 29 pM) and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. PD153035 exposure does not affect the expression of either EGF receptors or HER2/neu. PD153035 causes dose-dependent growth inhibition of EGF receptor-overexpressing cell lines at low micromolar concentrations, and the IC50 values in monolayer cultures at less than 1 μM in most cell lines tested.

EGFR: 6 pM (Ki); EGFR: 25 pM (IC₅₀)