Cbl-b-IN-29-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECbl-b-IN-29Cat.No.:HY-179575CASNo.:3070411-10-5分⼦式:C₃₀H₃₄FN₅O分⼦量:499.62作⽤靶点:E1/E2/E3Enzyme;InterleukinRelated作⽤通路:MetabolicEnzyme/Protease;Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Cbl-b-IN-29⼀种⼝服有效的CBL-B抑制剂。CBL-B结合活性⼝袋从⽽有效抑制免疫E3泛素连接酶的功能。Cbl-b-IN-29可以诱导Jurkat细胞释放IL-2(EC50=159nM)。Cbl-b-IN-29在体内表现出强⼤的抗肿瘤功效，且具有良好的耐受性，未观察到不良反应。Cbl-b-IN-29可⽤于癌症免疫治疗，结肠癌和肿瘤免疫联合的相关研究[1]。体外研究Cbl-b-IN-29(compound20)hasalowriskforCYPinhibition/inductionandhERGinhabitation[1].体内研究Cbl-b-IN-29(compound20)(30mg/kg,p.o.,oncedailyfor15days)exhibitsgoodanti-tumorefficacywithanimaltolerabilityandnoobservedadversereactionsinmurineCT26syngeneictumormousemodel,eitherasamonotherapyorinacombinationofanti-mousePD-1antibody(i.p.,twiceaweek)[1].AnimalModel:CT26tumorcells(3×105)-inducedBALB/cmice(6-8weeks)[1]Dosage:30mg/kgAdministration:p.o.,oncedailyfor15daysResult:Resultedinarobustanti-tumorefficacywithatumorgrowthinhibition(TGI)of76%.IndicatedalowriskforCYPinhibition/inductionandherginhibition.Exhibitedgoodanimaltolerability,withnoobservedadverse412reactions..REFERENCES1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].HanWang,etal.Aunifiedlanguagemodelbridgingdenovoandfragment-based3DmoleculedesigndeliverspotentCBL-Binhibitorsforcancertreatment.bioRxiv,2088260McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589