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Z-因多昔芬盐酸盐 /Endoxifen Z-isomer HCl {[allProObj[0].p_purity_real_show]}

货号:A506511 同义名: Endoxifen HCl;Endoxifen Z-isomer hydrochloride Ambeed 开学季,买赠积分,赢豪礼

Endoxifen Z-isomer HCl is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen Z-isomer HCl inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.

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Endoxifen Z-isomer HCl 化学结构 CAS号:1032008-74-4
Endoxifen Z-isomer HCl 化学结构
CAS号:1032008-74-4
Endoxifen Z-isomer HCl 3D分子结构
CAS号:1032008-74-4
Endoxifen Z-isomer HCl 化学结构 CAS号:1032008-74-4
Endoxifen Z-isomer HCl 3D分子结构 CAS号:1032008-74-4
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Endoxifen Z-isomer HCl 纯度/质量文件 产品仅供科研

货号:A506511 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide {[allProObj[0].p_purity_real_show]}
Glimepiride ++++

SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

{[allProObj[0].p_purity_real_show]}
Dronedarone Hydrochloride {[allProObj[0].p_purity_real_show]}
Gliquidone ++

Potassium channel, IC50: 27.2 nM

{[allProObj[0].p_purity_real_show]}
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

{[allProObj[0].p_purity_real_show]}
Glibenclamide {[allProObj[0].p_purity_real_show]}
Amiodarone HCl {[allProObj[0].p_purity_real_show]}
Gliclazide ++

Potassium channel, IC50: 184 nM

{[allProObj[0].p_purity_real_show]}
Repaglinide {[allProObj[0].p_purity_real_show]}
Dofetilide {[allProObj[0].p_purity_real_show]}
Nateglinide {[allProObj[0].p_purity_real_show]}
Quinine hydrochloride dihydrate {[allProObj[0].p_purity_real_show]}
ML133 HCl +

Kir2.1, IC50: 290 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Endoxifen Z-isomer HCl 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].

Endoxifen Z-isomer HCl 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

Endoxifen Z-isomer HCl 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.

Endoxifen Z-isomer HCl 实验方案

计算器
存储液制备 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

Endoxifen Z-isomer HCl 技术信息

CAS号1032008-74-4
分子式C25H28ClNO2
分子量 409.948
别名 Endoxifen HCl;Endoxifen Z-isomer hydrochloride
运输蓝冰
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

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