Pelitinib

Soluble in DMSO or ethanol. Pelitinib, also known as EKB 569, is a potent, irreversible inhibitor of the EGFR tyrosine kinase. Cell based IC(50) values range from 39nM to 80nM and in vitro kinase assays are in sub-nanomolar range for EGFR receptors. In xenograft tumor models using overexpressing A431 cells Pelitinib inhibits growth of tumors with effective doses of 3.5-10mg/kg/dl. Recent research also shows that Pelitinib can potentiate radiation induced killing of squamouse cell carcinoma via the inhibition of IR-induced NF-kappaB mediated cell survial pathway. Target: EGFR , Kinase Group: RTK , Substrate: Tyrosine