Antineoplastic Drug Gefitinib Powder CAS 184475-35-2 C22H24ClFN4O3

99% Antineoplastic Drug Gefitinib CAS 184475-35-2 with Best Price C22H24ClFN4O3

Product Name: Gefitinib
Synonyms: N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine Gefitinib;Gefitinib, >=99%;N-(3-Chlor-4-fluorophenyl)-7-[methoxy-6-[(3-morpholin-4-yl)propoxyl]-quinazolin-4-yl]amine;GEFITINIB RELATED COMPOUND;Gefitinib N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine;IRESSA;GEFITINIB;n-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
CAS: 184475-35-2
MF: C22H24ClFN4O3
MW: 446.9
EINECS: 643-034-7
Melting point: 119-120°C
Boiling point: 586.8±50.0 °C
Storage temp.: Store at RT

Description:

Geftinib is available as 250-mg tablets for oral administrationin the treatment of NSCLC for those patients who have failedto respond to platinum-based therapies and docetaxel and hasalso been used against squamous cell cancers of the head andneck. The agent is an inhibitor of the TK of EGF-R and possiblyother TKs as well.

Gefitinib is both a substrate and inhibitorof Pgp and BCRP. The agent is absorbed slowly afterbeing administered orally with 60% bioavailability.Metabolism occurs in the liver and is mediated primarily byCYP3A4 to give eight identified metabolites resulting fromdefluorination of the phenyl ring, oxidative-O-demethylation,and multiple products arising as a result of oxidation of themorpholine ring. The O-demethylated product represents thepredominate metabolite and is 14-fold less active comparedwith the parent. The parent and metabolites are eliminated inthe feces with a terminal elimination half-life of 48 hours.

The drug appears to be well tolerated with the most commonlyreported side effects being rash and diarrhea. It mayalso cause elevations in blood pressure especially in those patientswith preexisting hypertension, elevation of transaminaselevels, and mild nausea and mucositits.

Usage:

Gefitinib is an antineoplastic.