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Gefitinib

GEFITINIB
Product Number: C-1251

        

Details

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 prevalent in Asian populations.

Additional Information

Alternate Name/Synonyms Iressa, ZD1839
COA Documentation:
MP/BOILING POINT 586.8±50.0 °C at 760 mmHg
CHEMACX X1511922-9
Handling Room temperature
Package ID Refrigerated
INDICATION Non-Small Cell Lung Cancer
MDL NUMBER MFCD04307832
PACKING GROUP III
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
THERAPEUTIC AREA Oncological Disorders
UN #'S UN 3077
USE An EGFR-tyrosine kinase inhibitor use in cancer
Product Number C-1251
CAS # 184475-35-2
Chemical Name N-(3-chloro-4fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
Chemical Formula C22H24ClFN4O3
Appearance A crystalline Solid
Handling Room temperature
Melting Point 193-194 °C
Molecular Weight 446.9
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).
Storage Temp -20°C

Gefitinib