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Endoxifen

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Chemical Structure| 110025-28-0 同义名 : (E/Z)-N-desmethyl-4-hydroxy Tamoxifen;(E/Z)-Endoxifen
CAS号 : 110025-28-0
货号 : A155352
分子式 : C25H27NO2
纯度 : 97%
分子量 : 373.487
MDL号 : MFCD09840374
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 65 mg/mL(174.04 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The estrogen receptor (ER) is not only a powerful predictive and prognostic marker, but also an efficient target for the treatment of hormone-dependent breast cancer with antiestrogens[4]. Endoxifen is a potent antiestrogen that functions in part by targeting ERα for degradation by the proteasome in breast cancer cells[5]. Treatment of B16F10 mouse and SK-MEL-5 human melanoma cell lines with 10 μM of endoxifen for 48 h respectively resulted in 93.6 and 92.5% cell death. Orally administered endoxifen, at dose levels of 4 and 8 mg/kg body weight/day for 20 consecutive days, respectively reduced metastatic melanoma nodules in the lungs of B16F10 cell-bearing C57BL/6 mice by 26.7 and 82.7%[6]. Oral endoxifen administration once a day for 28 consecutive days at dosages 2, 4, and 8 mg/kg proved safe and resulted in progressive inhibition of the growth of the human mammary tumor xenografts in female mice making endoxifen a potentially new therapeutic agent for breast cancer[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.39mL

2.68mL

1.34mL

26.77mL

5.35mL

2.68mL
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 for degradation in breast cancer cells. Cancer Res. 2009 Mar 1;69(5):1722-7.

[3]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 Mar 1;69(5):1722-7.

[4]Sommer S, Fuqua SA. Estrogen receptor and breast cancer. Semin Cancer Biol. 2001 Oct;11(5):339-52.

[5]Wu X, Hawse JR, Subramaniam M, Goetz MP, Ingle JN, Spelsberg TC. The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells. Cancer Res. 2009 Mar 1;69(5):1722-7

[6]Chen P, Sheikh S, Ahmad A, Ali SM, Ahmad MU, Ahmad I. Orally administered endoxifen inhibits tumor growth in melanoma-bearing mice. Cell Mol Biol Lett. 2018 Jan 3;23:3.

[7]Ahmad A, Ali SM, Ahmad MU, Sheikh S, Ahmad I. Orally administered endoxifen is a new therapeutic agent for breast cancer. Breast Cancer Res Treat. 2010 Jul;122(2):579-84.