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Endoxifen Z-isomer hydrochloride
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。
Endoxifen Z-isomer hydrochloride图片
CAS NO:1032008-74-4
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Endoxifen HCl
Z-因多昔芬盐酸盐
产品介绍
Endoxifen HCl 是Tamoxifen最重要的代谢产物, 在表达ERα的乳腺癌细胞中发挥抗雌激素作用, Endoxifen HCl以浓度依赖的方式抑制HERG, IC50值为1.6μM。

产品描述

Endoxifen HCl is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.

体外活性

Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5]

体内活性

In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3]

细胞实验

MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.(Only for Reference)

Cas No.

1032008-74-4

分子式

C25H28ClNO2

分子量

409.95

别名

Endoxifen HCl;Z-因多昔芬盐酸盐

储存和溶解度

H2O:<1 mgml
Ethanol:69 mg/mL (168.3 mM)
DMSO:69 mg/mL (168.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years