PD153035

Description: PD153035 is reported to be a novel, potent, specific, and ATP competitive inhibitor of EGFR (Epidermal growth factor receptor) tyrosine kinase with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays, and to a lesser degree, of the closely related HER2/neu receptor; PD153035 inhibits 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 uM, 0.3 uM, 0.4 uM, 0.68 uM, 0.95 uM and 2.5 uM respectively. In addition, PD153035 could reverse ABCG2-mediated MDR in vitro (in human NSCLC and transfected cells overexpressing ABCG2) and in vivo. One of the major mediators of multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) is the overexpression of ATP-binding cassette subfamily G member 2 (ABCG2). Therefore, PD153035 may be a promising therapeutic strategy for NSCLC overexpressing ABCG2.

References: Science. 1994 Aug 19; 265(5175):1093-5; Invest New Drugs. 1996; 13(4):295-302. Cancer Lett. 2018 Jun 28; 424:19-29.

Related CAS: 183322-45-4 (HCl); 229476-53-3 ( EBE-A22, a derivative of PD 153035)