Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFLT3-IN-32Cat.No.:HY-174437CASNo.:3047195-48-9分?式:C??H??N?O?分?量:515.56作?靶點:FLT3;Apoptosis作?通路:ProteinTyrosineKinase/RTK;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性FLT3-IN-32?種強效的FLT3抑制劑。FLT3-IN-32對FLT3具有?選擇性，可有效抑制FLT3激活突變并誘導細胞凋亡(apoptosis)。FLT3-IN-32在?腫瘤??中表現(xiàn)出良好的耐受性。FLT3-IN-32在負荷MV4-11細胞的NOD/SCID??中顯?出卓越的抗腫瘤功效，能夠顯著延長??的?存期。FLT3-IN-32可?于急性髓系??病的研究[1]。體外研究FLT3-IN-32(Compound29c)(0.3-218.7nM,72h)effectivelyinhibitstheproliferationinfourdifferentBa/F3celllinesexpressingmutantFLT3isoforms[1].FLT3-IN-32showspromising(1μM-1M)selectivityandsafetytowardFLT3-ITD-positivecells[1].FLT3-IN-32(100-500nM,48h)inducesapoptosisinfourdifferentBa/F3celllinesexpressingmutantFLT3isoforms[1].FLT3-IN-32(1-50nM,4h)decreasesthelevelsofphosphorylationofFLT3anditsdownstreamsignalingmolecules(STAT5,MAPK)[1].CellProliferationAssay[1]CellLine:Ba/F3pMIYFLT3-ITD(NPOS),Ba/F3pMIYFLT3D835Y,Ba/F3pMIYFLT3NPOSD835Y,Ba/F3pMIYFLT3NPOSN676KcellsConcentration:0.3-218.7nMIncubationTime:72hResult:ShowedeffectivelyinhibitionwithIC50valuesof0.29nM,0.77nM,11.69nMand2.07nM,respectively.1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEApoptosisAnalysis[1]CellLine:Ba/F3pMIYFLT3-ITD(NPOS),Ba/F3pMIYFLT3D835Y,Ba/F3pMIYFLT3NPOSD835Y,Ba/F3pMIYFLT3NPOSN676KcellsConcentration:5,20,100,and500nMIncubationTime:48hResult:ShowedhighlypotentininducingapoptotsisinFLT3D835Ycells(54.11%)andFLT3NPOSN676Kcells(38.43%)at100nM.CellProliferationAssay[1]CellLine:Ba/F3pMIYFLT3-ITD(NPOS)cellsConcentration:1,5,10,20,and50nMIncubationTime:4hResult:DecreasedthelevelsofphosphorylationofFLT3anditsdownstreamsignalingmoleculesincludingSTAT5,MAPKandtoalesserextentalsoAKTinaconcentration-dependentmanner.體內(nèi)研究FLT3-IN-32(Compound29c)(50mg/kg,p.o.,dailyfor5days)showseffectivelytumorinhibitionMV4-11CDX(cell-linederivedxenograft)modelinnon-tumorbearingNOD/SCIDmice[1].AnimalModel:MV4-11CDX(cell-linederivedxenograft)modelinnon-tumorbearingNOD/SCIDmice(female,8-9weeks)[1]Dosage:50mg/kgAdministration:Oraladministration,dailyfor5daysResult:ShowedlessrelativebodyweightlosscomparedtoQuizartinib(HY-13001)andcomparablewithMidostaurin(HY-10230).ShowedsimilarlyinhibitiveactivityasQuizartinib(HY-13001)andmuchmoreactivethanMidostaurin(HY-10230).AnimalModel:Non-tumorbearingNOD/SCIDmice(female,6-8weeks)[1]Dosage:20,50,75mg/kgAdministration:Oraladministration,Intraperitonealinjection(20,50mg/kg),15daysResult:Showedgoodtolerability.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].SellmerA,etal.Novelwater-solubleandhighlyefficientdualtypeI/IInextgenerationinhibitorsofFMS-liketyrosinekinase3(FLT3).EurJMedChem.2025Jun8;296:117849.McePdfHeightCaution:Producthasnotbeenfullyvalidat