OP-1074-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOP-1074Cat.No.:HY-125263CASNo.:1443752-76-8分⼦式:C₂₉H₃₁NO₄分⼦量:457.56作⽤靶点:EstrogenReceptor/ERR作⽤通路:Others储存⽅式:-20°C,storedundernitrogen,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(218.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1855mL10.9275mL21.8551mL5mM0.4371mL2.1855mL4.3710mL10mM0.2186mL1.0928mL2.1855mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性OP-1074，纯抗雌激素药，⼀种选择性ER降解剂(PA-SERD)，对ERα和ERβ具有特异性抗雌激素活性，可抑制17β-estradiol(E2)-刺激的转录活性，IC50分别为1.6和3.2nM。IC50&TargetERαERβ体外研究OP-1074(0-100ꢀnM;24hours)inhibitsMCF-7cellsandCAMA-1cellsproliferationwithIC50valuesof6.3and9.2nM,respectively[1].OP-1074(100ꢀnM;24hours)destabilizatizesERαproteinexpressioninMCF-71/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEandCAMA-1cells[1].CellViabilityAssay[1]CellLine:MCF-7cells,CAMA-1cellsConcentration:0nM,10nM,100nMIncubationTime:24hoursResult:Inhibitedbreastcancercellproliferation.WesternBlotAnalysis[1]CellLine:MCF-7cells,CAMA-1cellsConcentration:100nMIncubationTime:24hoursResult:DownregulatedERαproteinexpression.REFERENCES[1].FanningSW,etal.SpecificstereochemistryofOP-1074disruptsestrogenreceptoralphahelix12andconferspureantiestrogenicactivity.NatCommun.2018Jun18;9(1):2368.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021