BBO-8520-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEBBO-8520Cat.No.:HY-158107CASNo.:2893809-51-1分子式:C₃₅H₃₃F₆N₇O₂S分子量:729.74作用靶点:Ras作用通路:GPCR/GProtein;MAPK/ERKPathway储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性BBO-8520是靶向KRASG12C的直接小分子共价抑制剂，同时具有KRASG12C(OFF)抑制剂特性和阻断KRASG12C(ON)信号的作用。BBO-8520通过将GTP结合蛋白锁定在状态1（一种无法结合效应子的构象）来抑制KRASG12C(ON)，从而抑制KRASG12C(ON)向下游发出的促细胞增殖的信号。BBO-8520还能快速且完全阻断RAS-RAF1相互作用，使KRASG12C回到非活性(OFF)状态。IC50&TargetKRASG12C[1]体外研究BBO-8520(10mg/kg/d;po)causesinhibitionofpERKandKRASG12CactivationinaKrasG12C-p53-drivenGEMMmodel,leadingtodurabletumorregression.BBO-8520alsodemonstratedstrongdose-andtime-dependentpharmacodynamiceffects(morethan80%inhibitionofpERK)inmicewithKRASG12Cmutanttumors[1].REFERENCESMaciagAE,etal.AbstractND07:BBO-8520,afirst-in-class,directinhibitorofKRASG12C(ON),locksGTP-boundKRASG12Cinthestate1conformationresultinginrapidandcompleteblockadeofeffectorbinding[J].CancerResearch,2024,84(7_Supplement):ND07-ND07.CaugheyBA,StricklerJH.TargetingKRAS-MutatedGastrointestinalMalignancieswithSmall-MoleculeInhibitors:ANewGenerationofBreakthroughTherapies[J].Drugs,2024,84(1):27-44.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792Fax:0