Endoxifen Z-isomer hydrochloride (Synonyms: Z-因多昔芬盐酸盐)
目录号: PL04830 纯度: ≥99%
CAS No. :1032008-74-4
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中文名称
Endoxifen Z-isomer hydrochloride
中文别名
4-[(1Z)-1-[4-[2-(甲基氨基)乙氧基]苯基]-2-苯基-1-丁烯-1-基]苯酚盐酸盐;Endoxifen (Z-isomer hydrochloride);Z-因多昔芬盐酸盐;HERG抑制剂(ENDOXIFEN Z-ISOMER HYDROCHLORIDE);内昔芬盐酸盐;ENDOXIFEN Z-异构体盐酸盐
英文名称
Endoxifen Z-isomer hydrochloride
英文别名
4-[(Z)-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol,hydrochloride;Endoxifen HCl;Endoxifen Z-isomer HCl;Endoxifen (hydrochloride);Endoxifen (Z-isomer hydrochloride);Endoxifen Z-isomer hydrochloride;CS-1633;Z-Endoxifen Hydrochloride
Cas No.
1032008-74-4
分子式
C25H27NO2.HCl
分子量
409.95
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Endoxifen Z-isomer hydrochloride盐酸盐是最重要的Tamoxifen代谢产物, 诱导在表达ERα的乳腺癌细胞中发挥抗雌激素作用, Endoxifen抑制hERG, 这种作用具有浓度依赖性, IC50值为1.6μM。
生物活性
Endoxifen Z-isomer hydrochloride 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 [1] Target: hERG Potassium Channel, Estrogen Receptor/ERR Endoxifen 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. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen tre
性状
Solid
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (121.97 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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