Gefitinib

Gefitinib is an EGFR inhibitor (IC50s = 0.023-0.079 µM). It inhibits colony formation of GEO colon, ZR-75-1 and MCF-10A breast, and OVCAR-3 ovarian cancer cell lines in soft agar assays (IC50s = 0.2-0.4 µM). Gefitinib (0.1 to 1 µM) induces apoptosis and inhibits EGFR autophosphorylation in the same cells. In vivo, gefitinib (1.25, 2.5, and 5 mg/kg) reduces tumor volume and increases survival in a GEO mouse xenograft model. Formulations containing gefitinib have been used in the treatment of non-small cell lung cancer (NSCLC).Formal Name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine. CAS Number: 184475-35-2. Synonyms: ZD 1839. Molecular Formula: C22H24ClFN4O3. Formula Weight: 446.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 205, 226, 250, 332 nm. SMILES: COC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4. 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). InChi Key: XGALLCVXEZPNRQ-UHFFFAOYSA-N.