Z-因多昔芬盐酸盐 T6827

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

相关产品: PHTPP | Endoxifen (Z-isomer) | XCT790 | FLTX1 | Enclomiphene citrate | Estradiol benzoate | WAY-200070 | Kaempferol | Estrogen receptor modulator 10 | Camizestrant TFA

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途