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• 产品描述： Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM. IC50 value: 1.6 μM Target: hERG Potassium Channel, Estrogen Receptor/ERR Endoxifen Z-isomer is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen Z-isomer observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen Z-isomer concentrations are needed when ERβ is absent.

• 靶点： Estrogen Receptor/ERR;Potassium Channel;EstrogenReceptor/ERR;Aromatase;Estrogen/progestogenReceptor;Parasite;DrugMetabolite

• 参考文献：
  1. Chae YJ, et al. Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels. Eur J Pharmacol. 2015 Apr 5;752:1-7. 2. Wu X, et al. Estrogen receptor-beta sensitizes breast cancer cells to the anti-estrogenic actions of endoxifen. Breast Cancer Res. 2011 Mar 10;13(2):R27.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃，避光

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.677 ml	13.387 ml	26.775 ml
  5 mM	0.535 ml	2.677 ml	5.355 ml
  10 mM	0.268 ml	1.339 ml	2.677 ml
  50 mM	0.054 ml	0.268 ml	0.535 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *