canertinib-hcl

Description: Canertinib (formerly also known as CI-1033; CI 1033; PD-183805) is a novel, potent and orally bioavailable quinazoline class of pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively. It has potential anticancer activity but it shows no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Canertinib binds to the intracellular domains of epidermal growth factor receptor tyrosine (ErbB) kinases irreversibly inhibiting their signal transduction functions and resulting in tumor cell apoptosis and suppression of tumor cell proliferation. This agent also acts as a radiosensitizing agent and displays synergistic activity with other chemotherapeutic agents.

References: J Med Chem. 2000 Apr 6; 43(7):1380-97; Semin Oncol. 2001 Oct; 28(5 Suppl 16):80-5.

Related CAS: 267243-28-7 (free base); 289499-45-2 (HCl)