PD-168393

PD-168393 is a potent, cell-permeable, irreversible, and selective small molecule inhibitor of the epidermal growth factor receptor (EGFR, also known as ErbB1) tyrosine kinase and ErbB2 (HER2/neu). It acts by covalently binding to the catalytic domain of EGFR at cysteine residue Cys773 within the ATP-binding pocket, thereby irreversibly inactivating EGFR tyrosine kinase activity. This results in inhibition of downstream signaling pathways involved in tumor cell proliferation. The compound demonstrates high selectivity for EGFR and ErbB2 over other kinases such as insulin receptor, platelet-derived growth factor receptor (PDGFR), fibroblast growth factor receptor (FGFR), and protein kinase C (PKC). Preclinical studies have shown anti-tumor activity in models of non-small cell lung cancer and other cancers with high EGFR expression. Developed originally by Warner-Lambert (later acquired by Pfizer), it remains an experimental tool compound without clinical approval[1][2][3][7].

Other names

4-[(3-bromophenyl)amino]-6-acrylamidoquinazolineN-(4-(3-Bromophenylamino)quinazolin-6-yl)acrylamideN-[4-[(3-Bromophenyl)amino]-6-quinazolinyl]-2-propenamide