N-Desmethyltamoxifen hydrochloride|15917-65-4|(三苯氧胺他莫昔芬EP杂质F HCl)-陌孚医药/Medlife

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N-Desmethyltamoxifen hydrochloride (Synonyms: 三苯氧胺他莫昔芬EP杂质F HCl)

目录号: PL09901 纯度: ≥99%

CAS No. :15917-65-4

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中文名称	N-Desmethyltamoxifen hydrochloride
中文别名	N-去甲基三苯氧胺盐酸盐;[(1S,2R)-1-苄基-2-羟基-3-[异丁基[(4-硝基苯基)磺酰]氨基]丙基]氨基甲酸叔丁酯;N-去甲基他莫昔芬盐酸盐;N-脱甲基他莫昔芬盐酸;枸橼酸他莫昔芬杂质F(EP) 标准品;他莫昔芬杂质;2-[4-[(1Z)-1,2-二苯基-1-丁烯基]苯氧基]-N-甲基乙胺盐酸盐;三苯氧胺他莫昔芬EP杂质F HCl
英文名称	N-Desmethyltamoxifen hydrochloride
英文别名	Ethanamine,2-[4-[(1Z)-1,2-diphenyl-1-butenyl]phenoxy]-N-methyl-, hydrochloride (9CI);N-DESMETHYL TAMOXIFEN HCL;N-Desmethyl Tamoxifen Hydrochloride;(Z)-2-(p-(1,2-Diphenyl-1-butenyl)phenoxy)-N-methylethylamine ICI 55,548;(Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N-methylethanamine Hydrochloride;N-Demethyltamoxifen Hydrochlorid;(Z)-2-(p-(1,2-Diphenyl-1-butenyl)phenoxy)-N-methylethylamine;ICI 55,548;N-Desmethyltamoxifen hydrochloride
Cas No.	15917-65-4
分子式	C₂₅H₂₇NO^.HCl
分子量	393.95
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	N-Desmethyltamoxifen hydrochloride 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 hydrochloride 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。
生物活性	N-Desmethyltamoxifen hydrochloride 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 hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
性状	Solid
IC50 & Target[1][2]	PKC
体外研究(In Vitro)	N-desmethyltamoxifen hydrochloride (20-500 ng/ml; 48 hours) has a profound inhibitory effect upon all seven glioma lines (T98G, U87, U138, U373, ALW, AUK, CAS cells). N-desmethyltamoxifen hydrochloride (1.5-10 μM; 114 hours) inhibits growth of MCF 7 human mammary carcinoma cells. N-desmethyltamoxifen hydrochloride, resulting from the CYP3A4/5-mediated catalysis of tamoxifen, is the major primary quantitative metabolite of tamoxifen. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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. [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.

溶解度数据	In Vitro: DMSO : 62.5 mg/mL (158.65 mM; Need ultrasonic)H₂O : 1 mg/mL (2.54 mM; ultrasonic and warming and heat to 60°C)配制储备液

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