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Endoxifen Z-isomer HCl

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Chemical Structure| 1032008-74-4 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 : 409.948
MDL号 : MFCD29049515
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(256.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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 活动说明 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.