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  3. N-Desmethyltamoxifen

N-Desmethyltamoxifen  (Synonyms: 他莫昔芬杂质F)

目录号: HY-129099
产品使用指南

N-Desmethyltamoxifen 是 Tamoxifen 在人体内的主要代谢产物。N-Desmethyltamoxifen,较弱的抗雌激素,是一种比 Tamoxifen 强十倍的蛋白激酶 C (PKC) 抑制剂。N-Desmethyltamoxifen 也是人体 AML 细胞神经酰胺代谢的有效调节因子,限制神经酰胺糖基化、水解和鞘氨醇磷酸化。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 N-Desmethyltamoxifen hydrochloride 通常具有更好的水溶性和稳定性。

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N-Desmethyltamoxifen Chemical Structure

N-Desmethyltamoxifen Chemical Structure

CAS No. : 31750-48-8

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N-Desmethyltamoxifen 的其他形式现货产品:

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].

IC50 & Target[1][2]

PKC

 

Estrogen Receptor

 

体外研究
(In Vitro)

N-desmethyltamoxifen (20-500 ng/ml; 48 hours) has a profound inhibitory effect upon all seven glioma lines (T98G, U87, U138, U373, ALW, AUK, CAS cells)[1].
N-desmethyltamoxifen (1.5-10 μM; 114 hours) inhibits growth of MCF 7 human mammary carcinoma cells[2].
N-desmethyltamoxifen, resulting from the CYP3A4/5-mediated catalysis of tamoxifen, is the major primary quantitative metabolite of tamoxifen[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: MCF 7 human mammary carcinoma cells
Concentration: 1.5, 2.5, 5, 7.5, 10 μM
Incubation Time: 114 hours
Result: Inhibits growth of MCF 7 human mammary carcinoma cells
分子量

357.50

Formula

C25H27NO

CAS 号
中文名称

他莫昔芬杂质F

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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N-Desmethyltamoxifen
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HY-129099
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