JAK2-IN-15-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEJAK2-IN-15Cat.No.:HY-178936CASNo.:3094174-82-7分子式:C₂₉H₃₅N₅O₄分子量:517.62作用靶点:JAK;STAT作用通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性JAK2-IN-15是一种口服有效的强效选择性JAK2抑制剂(IC50=1.17nM)。JAK2-IN-15可抑制AK2-STAT信号通路。在重组人促红素(rhEPO)诱导的小鼠模型中，JAK2-IN-15可显著改善血细胞比容和脾肿大等关键病理指标。JAK2-IN-15可用于真性红细胞增多症(PV)的研究[1]。IC50&TargetJAK21.17nM(IC50)体外研究JAK2-IN-15(Compound2)exhibitspotentJAK2inhibition(IC50=1.17nM)[1].JAK2-IN-15(72h)effectivelyinhibitstheproliferationofHEL(IC50=1.88μM)andSET-2(IC50=9.56μM)cellscarryingtheJAK2V617Fmutation[1].JAK2-IN-15(0.3-10μM,72h)exhibitssignificantantiproliferativeactivitiesagainstHELandSET-2cellswithJAK2V617FmutantbyinhibitingtheJAK2-STATsignalingpathwayinadose-dependentmanner[1].JAK2-IN-15(100μM)inhibitsonly17wild-typekinases,exhibitingstrongselectivity[1].WesternBlotAnalysis[1]CellLine:HEL92.1.7cells,SET-2Concentration:0.3μM,1μM,3μM,10μMIncubationTime:4hResult:EffectivelyinhibitedphosphorylationofJAK2(Y1007/8site),STAT3,STAT5,AKTand1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEERK.体内研究JAK2-IN-15(Compound2)(25-75mg/kg,p.o.,oncedailyfor4days)demonstratessignificanttherapeuticefficacyinamousemodelofrhEPO-inducedpolycythemia,dose-dependentlyinhibitingsplenomegaly,hematocrit,andreticulocytosis,withagoodsafetyprofile[1].AnimalModel:AmodelofpolycythemiaandsplenomegalywascreatedusingfemaleBALB/cmice(8-10weeksold,weighing17-20g)bysubcutaneousinjectionof10unitsofrecombinanthumanerythropoietin(rhEPO)dailyfor4consecutivedays[1].Dosage:25mg/kg,50mg/kg,75mg/kgAdministration:P.o.,oncedailyfor4daysResult:Spleenweightdecreased.Dose-dependentinhibitionofhematocrit.ReductionofrhEPO-inducedreticulocyteproliferation.InhibitionofTer119/CD71erythroblastexpansioninthespleenandbonemarrow.Nosignificanteffectonwhitebloodcellcountorbodyweight.REFERENCESHuF,etal.Exploringthemacrocyclicchemicalspaceforheuristicdrugdesignwithdeeplearningmodels.CommunChem.2025Oct7;8(1):299.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear