Gefitinib (ZD 1839)

Description: Gefitinib (formerly ZD1839, ZD-1839 or trade name: Iressa) is a potent and orally bioavailable EGFR inhibitor with potential anticancer activity. It inhibits EGFR Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib exhibits anti-angiogenic activities in a wide range of human tumor types, including head and neck, prostate, breast, ovarian, colon, small-cell lung and non-small-cell lung cancer. In May 2003, the FDA approved Gefitinib for non-small cell lung cancer (NSCLC). It was approved as monotherapy for the treatment of patients with locally advanced or metastatic NSCLC after failure of both platinum-based and docetaxel chemotherapies. i.e. as a third-line therapy.

References: Br J Cancer. 2005; 93(8):915-23.; Br J Cancer. 2002; 86(7): 1157–1161.; Clin Cancer Res. 2000; 6(12):4885-92.

Related CAS: 184475-55-6 (HCl salt)

Chemical Name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine

InChi Key: XGALLCVXEZPNRQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4, 11-14H, 2, 5-10H2, 1H3, (H, 25, 26, 27)

SMILES Code: COC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4CCOCC4