同义名 :	Endoxifen HCl; Endoxifen Z-isomer hydrochloride
	CAS号 :	1032008-74-4
	货号 :	A506511
	分子式 :	C25H28ClNO2
	纯度 :	99%+
	分子量 :	409.95
	MDL号 :	MFCD29049515
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Endoxifen Z-isomer hydrochloride, recognized as a pivotal Tamoxifen metabolite, plays a crucial role in delivering the anti-estrogenic effects of Tamoxifen in breast cancer cells that express estrogen receptor-alpha (ERα). It impedes hERG tail currents at 50 mV in a dose-responsive manner, with IC50 values established at 1.6 μM[1]. Furthermore, Endoxifen demonstrates greater potency in inhibiting estrogen target genes in the presence of ERβ. Notably, in patients treated with Tamoxifen exhibiting deficient CYP2D6 activity, low Endoxifen concentrations (20 to 40 nM) significantly reduce estrogen-induced cell proliferation rates when ERβ is expressed, contrasting with the higher concentrations required in the absence of ERβ[2].

细胞研究
细胞系	浓度	检测类型	检测时间	活性说明	数据源
MCF7 cells	10 uM	Function assay	6 h	Upregulation of ERalpha protein levels in human MCF7 cells at 10 uM after 6 hrs by Western blot method	24332630
MCF7:WS8 cells		Function assay	48 h	Agonist activity at ER in human MCF7:WS8 cells assessed as GREB1 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis	24805199

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.44mL 0.49mL 0.24mL	12.20mL 2.44mL 1.22mL	24.39mL 4.88mL 2.44mL

参考文献
[1]Chae YJ, et al. Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels. Eur J Pharmacol. 2015 Apr 5;752:1-7. [2]Wu X, et al. Estrogen receptor-beta sensitizes breast cancer cells to the anti-estrogenic actions of endoxifen. Breast Cancer Res. 2011 Mar 10;13(2):R27.