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。

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

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]

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

1032008-74-4

C25H28ClNO2

409.95

Endoxifen HCl;Z-因多昔芬盐酸盐

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