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 SMILES | OC1=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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. |