A major active metabolite of gefitinib in human plasma; inhibits EGFR in subcellular assays similarly to gefitinib (IC50s = 36 and 22 nM

O-Desmethyl Gefitinib – 1 mg

Brand:
Cayman
CAS:
847949-49-9
Storage:
-20
UN-No:
Non-Hazardous - /

O-Desmethyl gefitinib is the major metabolite of gefitinib (Item No. 13166) in human plasma, formed by the cytochrome P450 isoform CYP2D6.{39029} It is an active metabolite that inhibits EGFR similarly to gefitinib in subcellular assays (IC50s = 36 and 22 nM, respectively) but is less active in whole cell assays (IC50s = 760 and 49 nM, respectively).{39030} In a LoVo tumor mouse xenograft model, the tumor concentration of O-desmethyl gefitinib was 6.8-fold lower than that of gefitinib and did not significantly reduce tumor growth. A high plasma concentration of O-desmethyl gefitinib in patients homozygous for CYP2D6 was not associated with an increase in adverse effects.{39028}  

 

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Description

A major active metabolite of gefitinib in human plasma; inhibits EGFR in subcellular assays similarly to gefitinib (IC50s = 36 and 22 nM, respectively); less active than gefitinib in whole cell assays (IC50s = 760 and 49 nM, respectively); does not reduce tumor growth as well as gefitinib in a LoVo tumor mouse xenograft model,

Formal name: 4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]-7-quinazolinol

Synonyms: 

Molecular weight: 432.9

CAS: 847949-49-9

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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