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Over-activity of the epidermal growth factor receptor-associated tyrosine kinase (EGFR-TK) has been associated with a number of cancers and thus TK inhibitors could be potential therapeutic agents to prevent malignant growth. Gefitinib is a selective inhibitor of EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-Ras breast cancer, and OVCAR-3 ovarian cancer cell lines with ICs ranging between 0.2-0.4M. By interfering with the intracellular kinase domain, gefitinib prevents EGFR auto-phosphorylation and prevents downstream signal transduction. Gefitinib has been used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval for this compound (Iressa) when a phase III trial failed to demonstrate an overall survival benefit. Gefitinib appears to be most efficacious in treating certain EGFR gene mutations that are prevalsent in Asian populations.

Additional Information

Synonyms	Iressa, ZD1839
Product #	C-1251
CAS #	184475-35-2
Chemical Name	N-(3-chloro-4fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
Formula	C22H24ClFN4O3
MW	446.9
Appearance	A crystalline Solid
Purity	98%
Solubility	Soluble in ethanol (0.3 mg/ml), DMSO (20 mg/ml) or DMF (20 mg/ml), which should be purged of inert gas. Gefitinib is sparingly soluble in aqueous buffers.(For more information, please read Cof A).
Melting Point	193-194 °C
Storage Temp	-20°C
Therapeutic Area	Oncological Disorders
Use	An EGFR-tyrosine kinase inhibitor use in cancer

Additional Information

MDL Number	MFCD04307832
ChemACX	X1511922-9
InChI	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	COc1cc2c(cc1OCCCN3CCOCC3)c(ncn2)Nc4ccc(c(c4)Cl)F