Endoxifen-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEndoxifen hydrochlorideCat. No.: HY-18719BCAS No.: 1197194-41-4分式: CHClNO分量: 409.95作靶点: Estrogen Receptor/ERR作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 35 mg/mL (85.38 mM)*

2、means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4393 mL 12.1966 mL 24.3932 mL5 mM 0.4879 mL 2.4393 mL 4.8786 mL10 mM 0.2439 mL 1.2197 mL 2.4393 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Endoxifen hydrochlorideTamoxifen 的活性代谢物，有效的雌

3、激素受体 (estrogen receptor) 拮抗剂。IC50 & Target Estrogen receptor 1体外研究Endoxifen blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cellproliferation. These studies reveal that Endoxifen concentrations between 10 and 1000 nM enhance ER1/2 Master of Small Molecules 您边的抑制剂

4、师www.MedChemEprotein degradation. Lower concentrations of Endoxifen (1 nM) do not affect ER protein levels 1.体内研究 GLAST:Cre(ERT);ROSA26loxP/loxP mice are injected intraventricularly with 5 L 5 mM Endoxifen, and miceinjected with 4 L Adeno-Cre virus 109 plaque-forming units (pfu) serve as positive co

5、ntrol. At 7-10 daysafter ICV injection, mice are sacrificed and the SVZ dissected to isolate and derive stem and progenitor cells.These stem/progenitor cells are then cultured in permissive medium to form neurospheres and assayed forrecombination. In our unpassaged preparations is found derived from

6、 Endoxifen-injectedGLAST:CreERT2;ROSA26loxP/loxP mice that 1.9% of neurospheres show recombination, compared to ahigher rate of 4.3% of neurospheres in Adeno-Cre-recombined ROSA26loxP/loxP mice 2.PROTOCOLCell Assay 1 MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing

7、medium for 3 d. Thecells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated asindicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit 1.MCE has not independently

8、 confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 2 GLAST:CreERT2 mice are used. Tamoxifen is injected as active metabolite 4-hydroxytamoxifen (4-OH-TAM), or 4-hydroxy-N-desmethyltamoxifen (Endoxifen). 4-OH-TAM is dissolved at 1 mM concentration in 2%e

9、thanol/PBS and 5 L injected into the ventricles. Endoxifen has not been used before for the induction of theERT2 system. Endoxifen hydrochloride hydrate has a recommended solubility of over 10 mg/mL (25 mM) in100% DMSO, corresponding to a maximum concentration of 25 mM or a dose of 125 nmol in a 5 L

10、 volume.At this concentration, a proportion of mice developed neurological signs suggestive of neurotoxicity.Subsequently, concentrations of 2.5, 5, 10, 12.5 and 25 mM, dissolved in 10, 20, 40, 50 and 100% DMSO,respectively, corresponding to a drug dose of 12.5, 25, 50, 62.5 and 125 nmol are used. F

11、or testing DMSOtoxicity, groups of three mice are injected with 5 uL PBS, 50% DMSO in PBS or 100% DMSO in PBS. Miceare culled 9 days after injection and coronally sectioned brains are stained for cleaved caspase 3, GFAP andIba1.MCE has not independently confirmed the accuracy of these methods. They

12、are for reference only.REFERENCES1. Wu X, et al. The tamoxifen metabolite, Endoxifen, is a potent antiestrogen that targets estrogen receptor alpha fordegradation in breastcancer cells. Cancer Res. 2009 Mar 1;69(5):1722-7.2. Benedykcinska A, et al.Generation of brain tumours in mice by Cre-mediated recombination of neural progenitors in situ with thetamoxifen metabolite Endoxifen. Dis Model Mech. 2016 Feb;9(2):211-20.McePdfHeightCaut