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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
包装与价格:
包装价格(元)
500μg电议
1mg电议
5mg电议

产品介绍
O-去甲基吉非替尼是吉非替尼在人血浆中的活性代谢物。 O-去甲基吉非替尼的形成依赖于 CYP2D6 活性。 O-desmethyl gefitinib 在亚细胞试验中抑制 EGFR,IC50 为 36 nM。
Cas No.847949-49-9
别名O-去甲基吉非替尼
Canonical SMILESOC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4
分子式C21H22ClFN4O3
分子量432.9
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.