1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETamoxifenCat. No.: HY-13757ACAS No.: 10540-29-1Synonyms: ICI47699; Z-Tamoxifen; trans-Tamoxifen分式: CHNO分量: 371.51作靶點: Autophagy; Estrogen Receptor/ERR作通路: Autophagy; Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mont

2、hs-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 30 mg/mL (80.75 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.60 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (5.60 mM); Suspended solution; Need ultras

3、onic3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.60 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tamoxifen種選擇性雌激素受體調(diào)節(jié)劑 (SERM)，可阻斷乳腺細(xì)胞中的雌激素作，并可激活其他細(xì)胞，如骼，肝臟和宮細(xì)胞中的雌激素活性。IC50 & Target Estrogen receptor 1體外研究 Tamoxifen shows strong inhibition of MCF-7 cells (EC50=1.41 M) and to a lesser exte

4、nt the T47D cells(EC50=2.5 M) but does not affect the MDA-MB-231 cells 2.體內(nèi)研究 The Tamoxifen-inducible gene knockout strategy has clear advantages in that expression of a gene can beablated in adult mice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7-week oldTmcsMed1

5、-/- mice are given a daily Iintraperitoneal injection of Tamoxifen at a dose of 65 mg/kg for 5 daysand killed at selected intervals thereafter. qPCR analysis of RNA shows that the Med1 expression begin todecrease after 3 days of Tamoxifen injection (about 70% decrease), and by 5 days of injection, M

6、ed1expression is almost non-detectable in the heart. Tamoxifen-inducible cardiac-specific disruption of Med1(TmcsMed1-/-) in adult mice causes dilated cardiomyopathy 3.PROTOCOLAnimal Mice 3Administration 3 Seven-week old TmcsMed1-/- mice and the wild-type littermates are then administered Tamoxifeni

7、ntraperitoneally at a daily dose of 65 mg/kg body weight for 5 days and then killed at selected intervals afterinitiation of Tamoxifen treatment. For each experiment 3 to 5 mice for control and csMed1-/- are used. Toobtain survival curve 41 csMed1-/- and 41 csMed1fl/fl mice are used. Thirteen TmcsMe

8、d-/- mice and thesame number of littermates are used for the survival curve experiments using Tamoxifen inducible model.The specific criteria for animal euthanasia included absence of food or water intake, slow or no mobility,weak or absence of heart beat, absence of palpitation of the chest as well

9、 as absence of respiratorymovement. Mice are euthanized by intraperitoneal pentobarbital injection at the dose of 150mg/kg bodyweight to minimize suffering.MCE has not independently confirmed the accuracy of these methods. They are for reference only. Biomacromolecules. 2015 Sep 14;16(9):2701-14. Ce

10、ll Commun Signal. 2019 May 23;17(1):50. Chemosphere. 2019 Aug 29;239:124705. Am J Transl Res. 2018 Jul 15;10(7):2184-2194.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Osborne CK. Tamoxifen in the treatment of breast cancer. N

11、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) andassessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.3. Jia Y, et al. Cardiomyocyte-Specif

12、ic Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice.PLoS One. 2016 Aug 22;11(8):e0160755.4. Wang Y, et al. Evaluation of the safety and tolerability of tamoxifen for ischemia-incited renal injury in mice. Am J Transl Res. 2018 Jul15;10(7):2184-2194. eCollection 2018.McePdfHeightCaution: