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O-Desmethyl Gefitinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
O-Desmethyl Gefitinib图片
CAS NO:847949-49-9
规格:98%
分子量:432.9
包装与价格:
包装价格(元)
500ug电议
1mg电议
5mg电议

产品介绍
O-Desmethyl gefitinib is the major metabolite of gefitinib in human plasma, formed by the cytochrome P450 isoform CYP2D6.
CAS:847949-49-9
分子式:C21H22ClFN4O3
分子量:432.9
纯度:98%
存储:Store at -20°C

Background:

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.