Tamoxifen Citrate (Synonyms: ICI 46474, Istubal, Kessar, Noltam, Nolvadex, TMX, Valodex, Zemide) |
| رقم الكتالوجGC11669 |
تاموكسيفين سيترات (ICI 46474) هو مُعدِّل لمستقبلات الاستروجين الانتقائي النشط عن طريق الفم (SERM) الذي يمنع عمل هرمون الاستروجين في خلايا الثدي ويمكن أن ينشط نشاط هرمون الاستروجين في الخلايا الأخرى ، مثل خلايا العظام والكبد والرحمالمنشط ويعزز نشاط ATPase الموصوف الجزيئي Hsp90تاموكسيفين سيترات يثبط أيضًا العدوى EBOV Zaire و Marburg (MARV) مع IC من 0.1 ميكرومتر و 1.8 ميكرومتر ، على التواليتاموكسيفين سيترات ينشط الالتهام الذاتي ويحث على موت الخلايا المبرمج
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 54965-24-1
Sample solution is provided at 25 µL, 10mM.
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Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[4].
Tamoxifen Citrate (ICI 46474) shows strong inhibition of MCF-7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) but does not affect the MDA-MB-231 cells[2].
The Tamoxifen Citrate-inducible gene knockout strategy has clear advantages in that expression of a gene can be ablated in adult mice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7-week old TmcsMed1-/- mice are given a daily Iintraperitoneal injection of Tamoxifen Citrate at a dose of 65 mg/kg for 5 days and killed at selected intervals thereafter. qPCR analysis of RNA shows that the Med1 expression begin to decrease after 3 days of Tamoxifen Citrate injection (about 70% decrease), and by 5 days of injection, Med1 expression is almost non-detectable in the heart. Tamoxifen Citrate-inducible cardiac-specific disruption of Med1 (TmcsMed1-/-) in adult mice causes dilated cardiomyopathy[3].
References:
[1]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.
[2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.
[3]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.
[4]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.
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