PROTAC-AR-V7-degrader-2-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPROTACAR-V7degrader-2Cat.No.:HY-148771CASNo.:2488296-74-6分?式:C??H??F?N?O?S?分?量:882.05作?靶點:PROTACs;AndrogenReceptor;Apoptosis作?通路:PROTAC;VitaminDRelated/NuclearReceptor;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性PROTACAR-V7degrader-2?種于AR的PROTAC。PROTACAR-V7degrader-2通過降解AR-V7和AR-FL抑制CaP細胞增殖。PROTACAR-V7degrader-2誘導(dǎo)細胞凋亡(apoptosis)。體外研究PROTACAR-V7degrader-2(compound16;0-20μM;4d;22Rvlcells)inhibitscellgrowthindose-dependentmanner[1].PROTACAR-V7degrader-2(10μM;4d;22Rvlcells)reducesAR-V7proteinlevels[1].PROTACAR-V7degrader-2(1μM;0-48h;22Rvlcells)inducesapoptosisandincreasesannexin-Vstaining[1].CellViabilityAssay[1]CellLine:22RvlcellsConcentration:0-20μMIncubationTime:4daysResult:Reducedthecellcountbylessthan50percent.ApoptosisAnalysis[1]CellLine:22RvlcellsConcentration:1μM1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:0-48hResult:Inducedcellapoptosisin22Rvlcells.WesternBlotAnalysis[1]CellLine:22RvlcellsConcentration:10μMIncubationTime:4daysResult:ReducedAR-V7proteinlevels.體內(nèi)研究PROTACAR-V7degrader-2(compound16;2.5mg/mL;intratumorinjection)inhibitstumorgrowthinnu/numicewith22Rvl-EnzRtumorxenografts[1].AnimalModel:nu/numicewith22Rvl-EnzRtumorxenografts[1]Dosage:2.5mg/mLAdministration:intratumorinjectionResult:Inhibitedtumorgrowthinnu/numicewith22Rvl-EnzRtumorxenografts.REFERENCES[1].JennyD,et,al.Bi-functionalcompoundsandmethodsfortargetedubiquitinationofandrogenreceptor.WO2021236695.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792