ALK-IN-23-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEALK-IN-23Cat.No.:HY-151155分⼦式:C₂₆H₂₉ClN₈O₃S分⼦量:569.08作⽤靶点:Anaplasticlymphomakinase(ALK)作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性ALK-IN-23⼀种有效的ALK抑制剂，对ALKWT、ALKL1196M和ALKG1202R的IC50分别为1.6nM、0.71nM和1.3nM。ALK-IN-23可将细胞阻滞在G2期，并诱导细胞凋亡(apoptosis)。ALK-IN-23在体外抑制癌细胞迁移和集落形成。ALK-IN-23在H2228异种移植裸⿏模型中表现出抗良好的肿瘤活性与低毒性。IC50&TargetIC50:1.6nM(ALKWT),0.71nM(ALKL1196M),1.3nM(ALKG1202R)[1]体外研究ALK-IN-23(compoundY28)(0-5μM;72h)hashighlyinhibitoryactivityagainstH3122,H2228,Karpas299andA549[1].ALK-IN-23(25-100nM;3days)clearlyreducesthenumberofH2228cellcolonies,andalmostcompletelyabolishestheformationofcoloniesat100nM[1].ALK-IN-23(100-200nM;48h)facilitatestheapoptosisofH2228cells[1].ALK-IN-23(5-10nM;24and48h)iseffectivetoblockthemigrationofmostcellsatadoseof10nM[1].ALK-IN-23(25-100nM;overnight)significantlyincreasesthepercentageofcellsintheG2phase[1].CellProliferationAssay[1]CellLine:H3122,H2228,Karpas299andA549Concentration:0-5μMIncubationTime:72hResult:ExhibitedhighlyinhibitoryactivityagainstH3122,H2228,Karpas299andA549withIC50sof12nM,17nM,15nMand1.33μM.ApoptosisAnalysis[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:H2228cellsConcentration:100nM,200nMIncubationTime:48hResult:FacilitatedtheapoptosisofH2228cellsinadosedependentmannerandexhibitedamorepro-apoptoticeffectthanthatofCeritinib(HY-15656).CellMigrationAssay[1]CellLine:H2228cellsConcentration:5nMand10nMIncubationTime:24and48hResult:Blockedthemigrationofmostcellsatadoseof10nM(migrationrate:24h2.31%,48h:5.01%).CellCycleAnalysis[1]CellLine:H2228cellsConcentration:25nM,50nM,100nMIncubationTime:OvernightResult:SignificantlyincreasedthepercentageofcellsintheG2phasefrom11.28%to73.23%inadramaticdose-dependentmanner,accompaniedbyaresultantlossofG1-andS-phasepopulations.体内研究ALK-IN-23notesamoderatehalf-lifeof16.3minandahighintrinsicliverclearanceof152.9mL/min/kginrats[1].ALK-IN-23(25and50mg/kg;IG;onceevery2days;for14days)exhibitedgentleantitumorefficacyandnosignificantweightlossinH2228xenograftmicemodel[1].AnimalModel:FemaleBALB/cnudemice(5×106cellsH2228cellssuspendedinserum-freemediawereinjectedintotheflanks)[1]Dosage:25and50mg/kgAdministration:IG;onceevery2days;for14daysResult:Presentedmoderateantitumorefficacywiththetumorgrowthinhibition(TGI)of70.46%at50mg/kg.Possessedgentleantitumorefficacyandexhibitednosignificantweightloss.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].YangJ,etal.Design,synthesisandantitumorevaluationofATPdual-mimic2,4-diarylaminopyrimidineandaminoindazoleconjugatesaspotentanaplasticlymphomakinaseinhibitors.EurJMedChem.2022Jul31;241:114626.McePdfHeightCaution:Producthasnotbeenfullyvalid