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因多昔芬 /Endoxifen {[allProObj[0].p_purity_real_show]}

货号:A155352 同义名: (E/Z)-N-desmethyl-4-hydroxy Tamoxifen;(E/Z)-Endoxifen Ambeed 开学季,买赠积分,赢豪礼

Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity.

Endoxifen 化学结构 CAS号:110025-28-0
Endoxifen 化学结构
CAS号:110025-28-0
Endoxifen 3D分子结构
CAS号:110025-28-0
Endoxifen 化学结构 CAS号:110025-28-0
Endoxifen 3D分子结构 CAS号:110025-28-0
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Endoxifen 纯度/质量文件 产品仅供科研

货号:A155352 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Aromatase 其他靶点 纯度
Obacunone +

Aromatase, IC50: 28.4 μM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Endoxifen 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].

Endoxifen 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.

Endoxifen 实验方案

计算器
存储液制备 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

Endoxifen 技术信息

CAS号110025-28-0
分子式C25H27NO2
分子量 373.487
别名 (E/Z)-N-desmethyl-4-hydroxy Tamoxifen;(E/Z)-Endoxifen
运输蓝冰
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
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