Endoxifen hydrochloride (Synonyms: 因多昔芬盐酸盐)
目录号: PL04831 纯度: ≥98%
CAS No. :1197194-41-4
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中文名称
Endoxifen hydrochloride
中文别名
Endoxifen (hydrochloride);因多昔芬盐酸盐
英文名称
Endoxifen hydrochloride
英文别名
Endoxifen (hydrochloride);Endoxifen hydrochloride;Endoxifen HCl;Z-Endoxifen hydrochloride;308PA1L567;(Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol hydrochloride;Endoxifen Z-Isomer Hydrochloride;BCP24689;NSC750393;s7839;4-Hydroxy-N-desmethyl-tamoxifen, hydrochloride;Q27255933;(Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol hy
Cas No.
1197194-41-4
分子式
C25H28ClNO2
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 hydrochloride 是Tamoxifen 的关键活性代谢物,与雌激素受体 (estrogen receptor) 有较高的亲和力和特异性,同时也能抑制芳香酶的活性。Endoxifen hydrochloride 有用于乳腺癌研究的潜力。
生物活性
Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.
性状
Solid
IC50 & Target[1][2]
Aromatase
体外研究(In Vitro)
Endoxifen, a hydroxylated Tamoxifen metabolite, is approximately 100-fold more potent as an antagonist of the ER than tamoxifen. It also suggests that endoxifen but not 4-hydroxytamoxifen results in ER-alpha degradation in addition to its effects on the ER at the level of transcription. Endoxifen, is a potent antiestrogen that targets estrogen receptor α for degradation in breast cancer cells. Additionally, it is showed that Endoxifen blocks ERA transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation even in the presence of tamoxifen, N-desmethyl-tamoxifen, and 4-hydroxytamoxifen. Endoxifen is strongly growth inhibitory at 10 μM for all the breast cancer cell lines except for moderate inhibition for MDAMB-468.Cytotoxic effects are quite significant at 10 μM concentration for MCF7, HS 578T, and BT-549 cells. At lower Endoxifen concentrations (0.0
体内研究(In Vivo)
Orally administered Endoxifen is rapidly absorbed and systemically available when tested in female rats. The Endoxifen-treated rats show 787% higher exposure (AUC 0–∞ ) and 1,500% higher concentration (C max ) levels of Endoxifen when compared with Tamoxifen. Oral Endoxifen administration once a day for 28 consecutive days at dosages 2, 4, and 8 mg/kg proves safe and results in progressive inhibition of the growth of the human mammary tumor xenografts in female mice. has not independently confirmed the accuracy of these methods. They are for reference only.
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)
ClinicalTrial
参考文献
[1]. Goetz MP, et al. Tamoxifen, endoxifen, and CYP2D6: the rules for evaluating a predictive factor. Oncology (Williston Park). 2009 Dec;23(14):1233-4, 1236.
[2]. Wu X, et al. The tamoxifen metabolite, Endoxifen, is a potent antiestrogen that targets estrogen receptor alpha fordegradation in breast cancer cells. Cancer Res. 2009 Mar 1;69(5):1722-7.
溶解度数据
In Vitro: DMSO : ≥ 35 mg/mL (85.38 mM)H2O : 1 mg/mL (2.44 mM; ultrasonic and warming and heat to 80°C)
搜索质检报告(COA)

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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