Bavdegalutamide-ARV-110-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBavdegalutamideCat.No.:HY-138641CASNo.:2222112-77-6Synonyms:ARV-110分⼦式:C₄₁H₄₃ClFN₉O₆分⼦量:812.29作⽤靶点:AndrogenReceptor作⽤通路:Others储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:26.67mg/mL(32.83mM;ultrasonicandwarmingandadjustpHto3withHClandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.2311mL6.1554mL12.3109mL5mM0.2462mL1.2311mL2.4622mL10mM0.1231mL0.6155mL1.2311mL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(sealedstorage,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Bavdegalutamide(ARV-110)⼀种具有⼝服活性的，特异性的雄激素受体(AR)PROTAC类降解剂。Bavdegalutamide能促进AR的泛素化和降解，可⽤于前列腺癌的研究[1]。体外研究BavdegalutamidecompletelydegradesARinallcelllinestested,withanobserved50%degradationconcentration(DC50)<1nM[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBavdegalutamide(0.01nM-300nM)leadstoARdegradationinLNCaPcellsinadose-dependentmanner[1].Bavdegalutamide(10nM;0.5-24hours)leadstoARdegradationinVCaPcellsinatime-dependentmanner[2].Bavdegalutamide(10-1000nM)suppressestheexpressionoftheAR-targetgenePSA,inhibitsAR-dependentcellproliferation,andinducesapoptosisatlownanomolarconcentrations[2].Bavdegalutamide(0.01nM-100nM)degradesclinicallyrelevantmutantARproteins(WTAR,F876L,T877A,M896VandH874V),andretainsactivityinahighandrogenenvironment(R1881,100nM)inVCaPcells[2].体内研究Bavdegalutamide(oralgavage;1mg/kg;QD)exhibitsagreaterthan90%ARdegradationinvivo.InLNCaP,VCaPandprostatecancerpatientderivedxenograft(PDX)models,BavdegalutamidealsoexhibitssignificantinhibitionoftumorgrowthandARsignaling[2].Bavdegalutamide(oralgavage;3or10mpk;30days)demonstratesinvivoefficacyandreductionofAR-targetgeneexpressioninalongterm,castrate,enzalutamide-resistantVCaPtumormodel.TheTGIare70%and60%for3mpkand10mpkdosage.Respectively[2].REFERENCES[1].TaaviNeklesa,etal.ARV-110:AnandrogenreceptorPROTACdegraderforprostatecancer.AmericanAssociationforCancerResearch.2018.78(13):pp.5236.[2].TaaviKNeklesa,etal.ARV-110:anoralandrogenreceptorPROTACdegraderforprostatecancer.GUASCO2019McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For