Alrizomadlin-Standard-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAlrizomadlin(Standard)Cat.No.:HY-101518RCASNo.:1818393-16-6分⼦式:C₃₄H₃₈Cl₂FN₃O₄分⼦量:642.59作⽤靶点:MDM-2/p53;ReferenceStandards;E1/E2/E3Enzyme;Apoptosis作⽤通路:Apoptosis;Others;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Alrizomadlin(Standard)Alrizomadlin(HY-101518)的分析标准品。本产品⽤于研究及分析应⽤。Alrizomadlin(APG-115)⼀种⼝服活性⼩分⼦MDM2蛋⽩抑制剂,可与MDM2蛋⽩结合，IC50值和Ki值分别为3.8nM和1nM。Alrizomadlin可阻断MDM2与p53的相互作⽤并且以p53依赖性⽅式诱导细胞周期停IC50&TargetIC50:3.8nm(APG-115)[1]REFERENCES[1].AngeloAguilar,etal.4-((3′R,4′S,5′R)-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylicAcid(AA-115/APG-115):APotentandOrallyActiveMurineDoubleMinute2(MDM2)InhibitorinClinicalDevelopment.JMedChem.2017Apr13;60(7):2819–2839.[2].AWTolcheretal,AphaseIb/IIstudyofAPG-115incombinationwithMK-3475inpatientswithunresectableormetastaticmelanomasoradvancedsolidtumors,AnnOncol.2019Feb1;30(Supplement_1).pii:mdz027.[3].HanjieYieaal,AnovelsmallmoleculeinhibitorofMDM2-p53(APG-115)enhancesradiosensitivityofgastricadenocarcinoma,JExpClinCancerRes.2018May2;37(1):97.[4].ChenH,etal.Restorationofp53usingthenovelMDM2-p53antagonistAPG115suppressesdedifferentiatedpapillarythyroidcancercells.Oncotarget.2017Jun27;8(26):43008-43022.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589