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

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

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。

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

N-Desmethyltamoxifen Chemical Structure

CAS No. : 31750-48-8

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N-Desmethyltamoxifen 的其他形式现货产品:

N-Desmethyltamoxifen hydrochloride

N-Desmethyltamoxifen 相关产品

•同靶点产品:

•同靶点蛋白产品:

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

N-Desmethyltamoxifen 相关抗体:

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

31750-48-8
中文名称

他莫昔芬杂质F
结构分类
  • Alkaloids
  • Other Alkaloids
初始来源
  • 内源性代谢物
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
Data Sheet (536 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Vertosick FT Jr, et al. A comparison of the relative chemosensitivity of human gliomas to tamoxifen and n-desmethyltamoxifen in vitro. J Neurooncol. 1994;19(2):97-103.  [Content Brief]

    [2]. Morad SA, et al. Modification of sphingolipid metabolism by tamoxifen and N-desmethyltamoxifen in acute myelogenous leukemia–Impact on enzyme activity and response to cytotoxics. Biochim Biophys Acta. 2015 Jul;1851(7):919-28.  [Content Brief]

    [3]. Reddel RR,et al. N-desmethyltamoxifen inhibits growth of MCF 7 human mammary carcinoma cells in vitro. Eur J Cancer Clin Oncol. 1983 Aug;19(8):1179-81.  [Content Brief]

    [4]. Seong Hwan Kim,et al. Use of Antidepressants in Patients with Breast Cancer Taking Tamoxifen. J Breast Cancer. 2010 Dec;13(4):325-336.

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