GMB-805-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGMB-805Cat.No.:HY-180968CASNo.:2489876-41-5分⼦式:C₄₂H₄₆ClF₂N₉O₇S分⼦量:894.39作⽤靶点:PROTACs;Bcr-Abl作⽤通路:PROTAC;ProteinTyrosineKinase/RTK储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性GMB-805⼀种BCR-Abl靶向PROTAC降解剂，其在K562细胞中的DC50为30nM。GMB-805对K562细胞具有强效抗增殖活性，在动物体内展现出显著的抗肿瘤活性，且安全性特征优良。GMB-805可⽤于慢性髓系⽩⾎病的相关研究[1][2]。IC50&TargetBcr-Abl30nM(DC50)体外研究GMB-805(1-30000nM,24h)dose-dependentlydegradesBCR/AblproteininK562cellswithaDC50of30nMinK562cells[1].GMB-805(1μM,8h)inducesBCR/AblproteindegradationviatheproteasomeinK562cells[1].GMB-805(1000nM,24h)reducesVHL-dependentBCR/Ablandc-AblproteinlevelsinK562cells[1].GMB-805(3days)possessespotentantiproliferativeactivityagainsttheBCR-AbldrivencelllineK562withanIC50of169nM[1].WesternBlotAnalysis[1]CellLine:K562cellsConcentration:25,250and2500nMIncubationTime:24hResult:DemonstratedanenhancedabilitytoinduceBCR-Abldegradation.WesternBlotAnalysis[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:K562cellsConcentration:1μMIncubationTime:8hResult:ReducedBCR-AblandAblproteinexpression,andthiseffectwasrescuedbycotreatmentwithEpoxomicn(1μM)(HY-13821).ReducedBCR-AblandAblproteinexpression,andthiseffectwasnotrescuedbycotreatmentwithChloroquine(50μM)(HY-17589A).ReducedBCR-AblandAblproteinexpression,andthiseffectwasrescuedbycotreatmentwithPevonedistat(1μM)(HY-70062).体内研究GMB-805(200mg/kg,i.p.,onceadayfor3days)exhibitspotentanti-tumoractivitywithfavorablesafetyprofileinaK562xenograftmousemodel[1].AnimalModel:K562cellsinduced-athymicmice[1]Dosage:200mg/kgAdministration:i.p.,onceadayfor3daysResult:Showednosignificantincreaseintumorvolume.Notoxicityorweightlosswasobservedinthetreatedanimals.REFERENCES[1].BurslemGM,etal.ScaffoldhoppingenablesdirectaccesstomorepotentPROTACswithinvivoactivity.ChemCommun(Camb).2020Jun23;56(50):6890-6892.[2].ChenX,etal.Mightymini-PROTACs:anemergingclassofdegraders.EurJMedChem.2026Jan5;301:118202.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch