O-Desmethyl Gefitinib |
Catalog No.GC44491 |
O-데스메틸 제피티닙은 인간 혈장에서 제피티닙의 활성 대사산물입니다. O-desmethyl gefitinib의 형성은 CYP2D6 활성에 의존합니다. O-데스메틸 제피티닙은 세포하 분석에서 36nM의 IC50으로 EGFR을 억제합니다.
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Cas No.: 847949-49-9
Sample solution is provided at 25 µL, 10mM.
O-Desmethyl gefitinib is the major metabolite of gefitinib in human plasma, formed by the cytochrome P450 isoform CYP2D6. 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). 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.
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