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Endoxifen hydrochloride

产品编号 T6827L CAS 1197194-41-4

Endoxifen hydrochloride，Tamoxifen的主要活性代谢产物，具备较高的对雌激素受体(estrogen receptor)的亲和力和特异性，并能抑制芳香酶活性。它在乳腺癌研究中表现出潜在应用价值。

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Endoxifen hydrochloride Chemical Structure

Endoxifen hydrochloride, CAS 1197194-41-4

规格	价格/CNY	货期
5 mg	￥ 394	现货
10 mg	￥ 648	现货
25 mg	￥ 1,330	现货
50 mg	￥ 2,358	现货
100 mg	￥ 3,743	现货
1 mL * 10 mM (in DMSO)	￥ 437	现货

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其他形式的 Endoxifen hydrochloride:

选择批次

纯度: 99.08%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.
体外活性	Endoxifen, an hydroxylated metabolite of Tamoxifen, exhibits approximately 100-fold greater potency as an estrogen receptor (ER) antagonist compared to tamoxifen. Furthermore, it indicates that endoxifen, unlike 4-hydroxytamoxifen, induces degradation of ER-alpha in breast cancer cells in addition to its transcriptional effects on the ER.[1] Endoxifen acts as a potent antiestrogen that promotes the degradation of estrogen receptor α in breast cancer cells. Additionally, it has been demonstrated that endoxifen hinders ERA transcriptional activity and effectively suppresses estrogen-induced proliferation of breast cancer cells, even in the presence of tamoxifen, N-desmethyl-tamoxifen, and 4-hydroxytamoxifen.[2] Endoxifen exhibits significant growth inhibition at a concentration of 10 μM for all breast cancer cell lines, except for MDAMB-468, which shows moderate inhibition. At a concentration of 10 μM, cytotoxic effects are particularly prominent in MCF7, HS 578T, and BT-549 cells. In contrast, lower concentrations of Endoxifen (0.01-1 μM) result in less significant inhibitory effects compared to 10 μM. However, a concentration of 100 μM of Endoxifen is found to be lethal for all tested cells.[2]
体内活性	Endoxifen, when administered orally, is quickly absorbed and readily enters systemic circulation. Administering oral Endoxifen once daily for 28 consecutive days, at dosages of 2, 4, and 8 mg/kg, has demonstrated safety and progressive inhibition of human mammary tumor xenograft growth in female mice.[2]

分子量	409.95
分子式	C25H28ClNO2
CAS No.	1197194-41-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 0.9 mg/mL (2.2 mM), Sonication and heating to 80℃ are recommended.

DMSO: 31.5 mg/mL (76.8 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O / DMSO	1 mM	2.4393 mL	12.1966 mL	24.3932 mL	60.983 mL
DMSO	5 mM	0.4879 mL	2.4393 mL	4.8786 mL	12.1966 mL
	10 mM	0.2439 mL	1.2197 mL	2.4393 mL	6.0983 mL
	20 mM	0.122 mL	0.6098 mL	1.2197 mL	3.0492 mL
	50 mM	0.0488 mL	0.2439 mL	0.4879 mL	1.2197 mL

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参考文献

1. Goetz MP. Tamoxifen, endoxifen, and CYP2D6: the rules for evaluating a predictive factor. Oncology (Williston Park). 2009;23(14):1233-1236. 2. Wu X, et al. The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells. Cancer Res. 2009;69(5):1722-1727. 3. Gingery A, et al. The effects of a novel hormonal breast cancer therapy, endoxifen, on the mouse skeleton. PLoS One. 2014;9(5):e98219.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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