A selective EGFR-TK inhibitor that blocks the growth of GEO colon cancer

Gefitinib – 500 mg

Brand:
Cayman
CAS:
184475-35-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon, ZR-75-1, and MCF-10A Ha-ras breast, and OVCAR-3 ovarian cancer cell lines with IC50 values of 0.2-0.4 µM.{17856} By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.{17857} Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.{17858,17859}  

 

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Description

A selective 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 (IC50s = 0.2-0.4 µM); interferes with the intracellular kinase domain of the EGFR; used to treat advanced (or recurrent) non-small cell lung cancer

Formal name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine

Synonyms:  ZD 1839

Molecular weight: 446.9

CAS: 184475-35-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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