PD153035

PD153035 is a potent, ATP-competitive and selective small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an extremely low IC50 in the low picomolar to nanomolar range[1][4][7]. It competitively binds at the ATP site and suppresses EGFR autophosphorylation as well as EGFR-dependent signaling, leading to inhibition of cell proliferation and clonogenicity in EGFR-overexpressing tumor cell lines[1][4][7]. While PD153035 can also inhibit HER2/neu (ErbB2) tyrosine kinase activity, it does so with significantly less potency[4][7]. Preclinical studies show anti-proliferative effects are closely correlated to EGFR expression levels. PD153035 is also used as a PET imaging probe when radio-labeled, e.g., with carbon-11, for in vivo imaging of EGFR expression in tumors[3][6]. In metabolic disease models, PD153035 demonstrates anti-inflammatory effects through modulation of macrophage polarization and improves glucose tolerance and insulin sensitivity, likely through EGFR inhibition[1][9]. This compound is considered a chemical probe and research tool and does not have clinical approval status.

Other names

4-(3-Bromoanilino)-6,7-dimethoxyquinazoline