Background:

PD153035 (4-(3-Bromoanilino)-6,7-dimethoxyquinazoline) is an extremely potent epidermal growth factor receptor (EGFR) inhibitor that competitively binds at the ATP site with the half maximal inhibition concentration IC50 of 0.025 nM resulting in the inhibition of the tyrosine kinase activity of the EGFR [1].

PD153035 has been found to inhibit EGF-dependent EGFR phosphorylation in a variety of human cancer cell lines over-expressing EGFRs, which include A431, Difi, DU145, MDA-MB-468, ME180 and C4i, with IC50 of 0.22 μM, 0.3 μM, 0.4 μM, 0.68 μM, 0.95 μM and 2.5 μM respectively leading to suppression of proliferation and clonogenicity in those cell lines [2].

Besides exerting potent inhibition against EGFRs, PD153035 also inhibits the closely related HER2/neu receptor but to a lesser degree [2].

参考文献:
[1] Bridges AJ, Zhou H, Cody DR, Rewcastle GW, McMichael A, Showalter HD, Fry DW, Kraker AJ, Denny WA. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.
[2] Bos M, Mendelsohn J, Kim YM, Albanell J, Fry DW, Baselga J. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106.