同义名 :	4-羟基三苯氧胺（Z异构体） ;trans-4-Hydroxytamoxifen; (Z)-Afimoxifene; ICI 79280; 4-Monohydroxytamoxifen; (Z)-4-OHT; (Z)-4-Hydroxytamoxifen
	CAS号 :	68047-06-3
	货号 :	A309666
	分子式 :	C26H29NO2
	纯度 :	99%+
	分子量 :	387.51
	MDL号 :	MFCD00278780
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Estrogen receptors (ERs) play a key role in breast cancer progression. It is reported that 75% of women diagnosed with breast cancer have estrogen and progesterone receptor-positive breast tumors[3]. 4-Hydroxytamoxifen (Afimoxifene, 4-OH-tamoxifen) is the active metabolite of tamoxifen and a selective estrogen receptor modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer. 1 µM of 4-OH-tamoxifen treatment for 1h inhibited LM05-E and MCF-7 cells proliferation, and this effect was related to the PI3K/AKT pathway[4]. In the MCF-7:5C cells, addition of 4-OH-tamoxifen at an equimolar concentration at early time points almost completely reversed the apoptosis induced by ethoxytriphenylethylene (10-6 M) after 1 and 2 days of treatment[5]. In vivo, three daily doses of 4-OH-tamoxifen (6 mg/day) effectively attenuated methamphetamine-induced nigrostriatal dopamine depletions in both sexes of intact and gonadectomized C57BL/6 J mice[6].

细胞研究
细胞系	浓度	检测类型	检测时间	活性说明	数据源
african green monkey Vero cells		Proliferation assay	72 h	Antiproliferative activity against african green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50=15.1 μM	25993269
BT-20 cells		Proliferation assay		Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration	2769681
Calu-1 cells		Function assay	30 mins	Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis, IC50=4.8 μM	19136975

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.58mL 0.52mL 0.26mL	12.90mL 2.58mL 1.29mL	25.81mL 5.16mL 2.58mL

参考文献

[1]Zhong Q, Zhang C, et al. Boronic prodrug of 4-hydroxytamoxifen is more efficacious than tamoxifen with enhanced bioavailability independent of CYP2D6 status. BMC Cancer. 2015 Sep 9;15:625. [2]Asp ML, Martindale JJ, et al. Direct, differential effects of tamoxifen, 4-hydroxytamoxifen, and raloxifene on cardiac myocyte contractility and calcium handling. PLoS One. 2013 Oct 24;8(10):e78768. [3]Raffo D, Pontiggia O, Bal de Kier Joffé E, Simian M. Non-genomic actions of estradiol and 4-OH-tamoxifen on murine breast cancer cells. Oncol Rep. 2015 Jan;33(1):439-47. doi: 10.3892/or.2014.3558. Epub 2014 Oct 22. PMID: 25338647. [5]Maximov PY, Abderrahman B, Fanning SW, Sengupta S, Fan P, Curpan RF, Rincon DMQ, Greenland JA, Rajan SS, Greene GL, Jordan VC. Endoxifen, 4-Hydroxytamoxifen and an Estrogenic Derivative Modulate Estrogen Receptor Complex Mediated Apoptosis in Breast Cancer. Mol Pharmacol. 2018 Aug;94(2):812-822. doi: 10.1124/mol.117.111385. Epub 2018 May 8. PMID: 29739819; PMCID: PMC6022805. [6]Kuo YM, Chen HH, Shieh CC, Chuang KP, Cherng CG, Yu L. 4-Hydroxytamoxifen attenuates methamphetamine-induced nigrostriatal dopaminergic toxicity in intact and gonadetomized mice. J Neurochem. 2003 Dec;87(6):1436-43. doi: 10.1046/j.1471-4159.2003.02089.x. PMID: 14713299.