Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.

ERG (human):1.6 μM

Endoxifen表现出抗雌激素效应，并降低E2诱导的PR表达在MCF-7细胞中。[1] Endoxifen还阻断ER-alpha的转录活性，并抑制由雌激素引起的乳腺癌细胞增殖。[2] 在MCF7、HS 578T和BT-549细胞中，Endoxifen显著抑制细胞增殖。[3] 与tamoxifen相比，Endoxifen在抑制PKC活性方面具有四倍的抑制效果。[4] Endoxifen通过优先与克隆的hERG钾通道的激活状态相互作用，抑制hERG电流，其IC50为1.6 μM。[5]

在体内，Endoxifen（8 mg/kg）能够抑制小鼠体内MCF-7人乳腺肿瘤异种移植物的生长，其效力超过Tamoxifen。[3]

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)