Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPROTACERαDegrader-11Cat.No.:HY-174870分子式:C??H??F?N?O??S分子量:997作用靶點(diǎn):PROTACs;EstrogenReceptor/ERR;Apoptosis;FluorescentDye作用通路:PROTAC;VitaminDRelated/NuclearReceptor;Apoptosis;Others儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PROTACERαDegrader-11是一種選擇性且具有內(nèi)源熒光(Ex:366nm,Em:440nm)的ERαPROTAC降解劑。PROTACERαDegrader-11在MCF-7乳腺癌細(xì)胞系中展現(xiàn)出良好的抗增殖活性、選擇性ERα降解能力及熒光成像功能。PROTACERαDegrader-11可以誘導(dǎo)MCF-7細(xì)胞G2/M期阻滯和凋亡(apotosis)。PROTACERαDegrader-11在無(wú)胸腺裸鼠中表現(xiàn)出良好的安全性，500mg/kg劑量下未見(jiàn)急性毒性反應(yīng)。PROTACERαDegrader-11可用于乳腺癌相關(guān)研究。(粉色：ERα配體：(HY-167701)，藍(lán)色：CRBN配體(HY-150831)，黑色：連接子，E3連接酶配體-連接子偶聯(lián)物：HY-174880)[1]。IC50&TargetERαERβ體外研究PROTACERαDegrader-11(CompoundW2)(96h)exhibitsexcellentcellinhibitoryactivitywithIC50valuesof0.19μM(MCF-7),1.40μM(MCF-7EGFR),4.31μM(MCF-7D538G)and9.29μM(MCF-7Y537S)[1].PROTACERαDegrader-11(10μM,0-24h)degradesERαinMCF-7cellsinatime-dependentmannerwithin24h,whichisreducedaftertheadditionoftheERαligand(OBHSA)(HY-167701)orCRBNligand[1].PROTACERαDegrader-11(0.5-10μM,24h)doesnotdegradeERβinPC9cells[1].PROTACERαDegrader-11(0-80μM,10-360min)exhibitsaconcentration-dependentandtime-dependentproportionalincreaseinfluorescenceintensity[1].PROTACERαDegrader-11(1-20μM,48h)inducesG2/MphasearrestandinducesapoptosisinMCF-7cells[1].PROTACERαDegrader-11(10μM,0-60min)exhibitshighphotostabilityinthepresenceofERα[1].PROTACERαDegrader-11(0.1-20μM)doesnotinducesignificantdamagetothebloodcellmembranesinSDrats[1].CellCycleAnalysis[1]1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:MCF-7cellsConcentration:1,10μMIncubationTime:48hResult:InducedG2/Mphasearrestdose-dependentlyinMCF-7cells.ApoptosisAnalysis[1]CellLine:MCF-7cellsConcentration:10,20μMIncubationTime:48hResult:Inducedapoptosisdose-dependentlyinMCF-7cells.體內(nèi)研究PROTACERαDegrader-11(CompoundW2)(500mg/kg,i.p.singledose)iswell-tolerateduptoadoseof500mg/kgwithnoacutetoxicityinathymicnudemice[1].AnimalModel:FemaleBALB/Cnudemice(5weeks)[1]Dosage:500mg/kgAdministration:i.p.forsingledoseResult:Showednotreatment-relatedmortalityorclinicalsignsoftoxicity(includingpiloerection,lethargy,orneurologicalabnormalities).Showednoabnormalityofbodyweightchanged.REFERENCESWuY,etal.DiscoveryofERα-targetingPROTACswithintrinsicfluorescenceforprecisiontheranosticsofbreastcancer.RSCMedChem.2025May22.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic