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- 產(chǎn)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.
- 靶點： Estrogen Receptor/ERR;Potassium Channel
- 參考文獻：
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.
- 溶解度： Soluble in DMSO
- 保存條件： 2-8℃，避光
- 配置溶液濃度參考：
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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