货号	规格	价格	上海	北京	珠海	重庆	武汉
S82288-5mg	≥98%	￥410.00 S82288-5mg ￥410.00 3-5天	0 货期：3-5天	-	-	-	-
S82288-10mg	≥98%	￥660.00 S82288-10mg ￥660.00 3-5天	0 货期：3-5天	-	-	-	-
S82288-50mg	≥98%	￥2310.00 S82288-50mg ￥2310.00 3-5天	0 货期：3-5天	-	-	-	-
S82288-100mg	≥98%	￥3710.00 S82288-100mg ￥3710.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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

靶点：

Aromatase

体外研究：

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 (0.01-1 μM), the inhibitory effects are not as significant as 10 μM, whereas 100 μM Endoxifen concentration found to be lethal for all tested cells

体内研究：

Orally administered Endoxifen is rapidly absorbed and systemically available when tested in female rats. The Endoxifen-treated rats show 787% higher exposure (AUC0–∞) and 1,500% higher concentration (Cmax) 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

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.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.439 ml	12.197 ml	24.393 ml
5 mM	0.488 ml	2.439 ml	4.879 ml
10 mM	0.244 ml	1.22 ml	2.439 ml
50 mM	0.049 ml	0.244 ml	0.488 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

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

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计算重置

Endoxifen (hydrochloride)