Product Introduction
Bioactivity


英文名: Endoxifen Z-isomer hydrochloride

描述: Endoxifen Z-isomer hydrochloride (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。

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)

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : <1 mg/mL
Ethanol : 69 mg/mL (168.3 mM)
DMSO : 69 mg/mL (168.3 mM)


关键字: inhibit | Inhibitor | Estrogen Receptor/ERR | Endoxifen Z-isomer Hydrochloride | Potassium Channel | KcsA | Endoxifen Z-isomer | Endoxifen Z isomer hydrochloride | Endoxifen Zisomer hydrochloride

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