N4-(3-Bromophenyl)-N6-methylpyrido[34-d]pyrimidine-46-diamine

PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM 49 52 52 nM for EGFR ErbB2 ErbB3 and ErbB4 respectively.

For R&D use onlynot for drug household or other uses.

A potent inhibitor of the EGFR tyrosine kinase activity (8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC5049 nM) and MDA-MB-453 (IC50 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 12 (MKK12) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells.