AKN-028-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAKN-028Cat.No.:HY-118304CASNo.:1175017-90-9分⼦式:C₁₇H₁₄N₆分⼦量:302.33作⽤靶点:FLT3;Caspase作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性AKN-028具有⼝服活性的酪氨酸激酶的抑制剂(TKI)，FLT3的抑制剂，其IC50值为6nM。AKN-028可剂量依赖性的诱导FLT3的⾃磷酸化。IC50&TargetCaspase3FLT3CLK1RPS6KA6nM(IC50)140nM(IC50)220nM(IC50)FGFR2VEGFR21200nM(IC50)520nM(IC50)体外研究AKN-028triggersapoptosisinMV4-11byactivationofcaspase3[1].AKN-028(10μM)iscytotoxictoAMLcelllinesandinducesapoptosisintheAMLcelllineMV4-11[1].CellCytotoxicityAssay[1]CellLine:AMLcelllineMV4-11.Concentration:10μM.IncubationTime:24h.Result:WascytotoxictoprimaryAMLcells,irrespectiveofFLT3mutationstatusandquantitativeFLT3expression.体内研究AKN-028(15ꢀmg/kg,Subcutaneouslyinjectiontwicedaily)exhibitsanti-tumoractivitiesforacutemyeloid1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEleukemia(AML)models[1].AnimalModel:MicebasedAMLandMV4-11cells[1].Dosage:15ꢀmg/kg.Administration:Subcutaneouslyinjectiontwicedaily.Result:InhibitednetgrowthofoneoftheprimaryAMLsamples(UPN26)invivoandfurthermorereducedthetumormassofMV4-11cellline.REFERENCES[1].AEriksson,etal.TheNovelTyrosineKinaseInhibitorAKN-028HasSignificantAntileukemicActivityinCellLinesandPrimaryCulturesofAcuteMyeloidLeukemia.BloodCancerJ.2012Aug3;2(8):e81.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589