HPK1-IN-65-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHPK1-IN-65Cat.No.:HY-179338分⼦式:C₂₃H₂₂ClFN₈O₂S分⼦量:528.99作⽤靶点:MAP4K;HOXA;InterleukinRelated作⽤通路:MAPK/ERKPathway;CellCycle/DNADamage;Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性HPK1-IN-65⼀种选择性且具有⼝服活性的HPK1抑制剂IC50值⼩于5nM，并对MAP4K激酶家族成员GLK表现出1257倍的选择性。HPK1-IN-65抑制pSLP76磷酸化的IC50为92.3nM。HPK1-IN-65刺激IL-2⽣成的EC50为398nM。HPK1-IN-65以剂量依赖的⽅式抑制TCR诱导的SLP76Ser376位点的磷酸化。HPK1-IN-65可进⼀步⽤于结肠癌研究[1]。IC50&TargetHPK1IL-250)398nM(EC50)体外研究HPK1-IN-65(compound34)decreasespSLP76inadose-dependentmannerinJurkatcelllinewithIC50valuesof92.3nM[1].HPK1-IN-65stimulatesIL-2productionwithanEC50of398nMandenhancestheactivationupto3.59fold[1].HPK1-IN-65hastheantiproliferativeeffectinJurkatcells[1].HPK1-IN-65hasselectivityagainstMAP4K2,MAP4K3,MAP4K4,MAP4K5,MAP4K6[1].体内研究HPK1-IN-65(compound34)(60mg/kg,p.o.,oncedailyfor14consecutivedays)exhibitsarobustantitumorresponseintheCT26syngeneictumormodelinfemaleBALB/cmice(6weeksold)[1].AnimalModel:ColorectalcarcinomacelllineCT-26cells(2.5×105cells,s.c.)inducedfemaleBALB/cmice(6-week-old)[1]Dosage:60mg/kgAdministration:i.g.,oncedailyfor14consecutivedays,Anti-PD-1monoclonalantibody(HY-P99709)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE(i.p.,10mg/kg,twiceaweek)Result:Achievedarobustanti-tumorresponsewithaTGIof62.90%.Causednosignificantimpactonanimalbodyweightineithermonotherapyorcombinationgroups.Delayedthetumorgrowth,withthetumorgrowthinhibition(TGI)reaching41.73%at14dayspost-treatment(withoutAnti-PD-1monoclonalantibody).REFERENCES[1].HuangW,etal.,DiscoveryofhighlyselectiveandpotentHPK1inhibitorsforcancerimmunotherapy.EurJMedChem.2026Jan15;302(Pt2):118322.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: