EzatiostatisaLiposomalsmall-moleculeglutathioneanaloginhibitorofglutathioneS-transferase(GST)P1-1withhematopoiesis-stimulatingactivity.Afterintracellularde-esterification,theactiveformofezatiostatbindstoandinhibitsGSTP1-1,therebyrestoringJunkinaseandMAPKpathwayactivitiesandpromotingMAPK-mediatedcellularproliferationanddifferentiationpathways.Thisagentpromotestheproliferationandmaturationofhematopoieticprecursorcells,granulocytes,monocytes,erythrocytesandplatelets.Checkforactiveclinicaltrialsorclosedclinicaltrialsusingthisagent.(NCIThesaurus).MedKooCat#:201360Name:EzatiostatCAS#:168682-53-9(freebase)ChemicalFormula:C27H35N3O6SExactMass:529.22466MolecularWeight:529.6483ElementalAnalysis:C,61.23;H,6.66;N,7.93;O,18.12;S,6.05Synonym:TLK199;TLK-199;TLK199;Ezatiostat;Brandname:TELINTRAIUPAC/ChemicalName:(S)-ethyl2-amino-5-(((R)-3-(benzylthio)-1-(((S)-2-ethoxy-2-oxo-1-phenylethyl)amino)-1-oxopropan-2-yl)amino)-5-oxopentanoateInChiKey:GWEJFLVSOGNLSS-FIXSFTCYSA-NInChiCode:InChI=1S/C27H35N3O6S/c1-3-35-26(33)21(28)15-16-23(31)29-22(18-37-17-19-11-7-5-8-12-19)25(32)30-24(27(34)36-4-2)20-13-9-6-10-14-20/h5-14,21-22,24H,3-4,15-18,28H2,1-2H3,(H,29,31)(H,30,32)/t21-,22-,24-/m0/s1SMILESCode:O=C(OCC)[C@@H](N)CCC(N[C@@H](CSCC1=CC=CC=C1)C(N[C@@H](C2=CC=CC=C2)C(OCC)=O)=O)=OTechnicalDataAppearance:WhitesolidpowderPurity:>98%(orrefertotheCertificateofAnalysis)CertificateofAnalysis:ViewCoA,currentbatch,Lot#CRB40225QCData:ViewQCdata:currentbatch,Lot#CRB40225.SafetyDataSheet(MSDS):ViewMaterialSafetyDataSheet(MSDS)ShippingCondition:Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.StorageCondition:Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).Solubility:SolubleinDMSO,notinwaterShelfLife:>2yearsifstoredproperlyDrugFormulation:ThisdrugmaybeformulatedinDMSOStockSolutionStorage:0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).HarmonizedSystemCode:293490AdditionalInformationRelatedCAS#168682-53-9(Ezatiostat);286942-97-0(EzatiostatHClsalt) References1:GaliliN,TamayoP,BotvinnikOB,MesirovJP,BrooksMR,BrownG,RazaA.Predictionofresponsetotherapywithezatiostatinlowerriskmyelodysplasticsyndrome.JHematolOncol.2012May6;5:20.doi:10.1186/1756-8722-5-20.PubMedPMID:22559819;PubMedCentralPMCID:PMC3407785.2:RazaA,GaliliN,MulfordD,SmithSE,BrownGL,SteensmaDP,LyonsRM,BocciaR,SekeresMA,Garcia-ManeroG,MesaRA.Phase1dose-rangingstudyofezatiostathydrochlorideincombinationwithlenalidomideinpatientswithnon-deletion(5q)lowtointermediate-1riskmyelodysplasticsyndrome(MDS).JHematolOncol.2012Apr30;5:18.doi:10.1186/1756-8722-5-18.PubMedPMID:22546242;PubMedCentralPMCID:PMC3416694.3:LyonsRM,WilksST,YoungS,BrownGL.OralezatiostatHCl(Telintra®,TLK199)andidiopathicchronicneutropenia(ICN):acasereportofcompleteresponseofapatientwithG-CSFresistantICNfollowingtreatmentwithezatiostat,aglutathioneS-transferaseP1-1(GSTP1-1)inhibitor.JHematolOncol.2011Nov2;4:43.doi:10.1186/1756-8722-4-43.PubMedPMID:22047626;PubMedCentralPMCID:PMC3235963.4:RazaA,GaliliN,SmithSE,GodwinJ,BocciaRV,MyintH,MahadevanD,MulfordD,RarickM,BrownGL,SchaarD,FaderlS,KomrokjiRS,ListAF,SekeresM.Aphase2randomizedmulticenterstudyof2extendeddosingschedulesoforalezatiostatinlowtointermediate-1riskmyelodysplasticsyndrome.Cancer.2012Apr15;118(8):2138-47.doi:10.1002/cncr.26469.Epub2011Sep1.PubMedPMID:21887679.5:QuddusF,ClimaJ,SeedhamH,SajjadG,GaliliN,RazaA.OralEzatiostatHCl(TLK199)andMyelodysplasticsyndrome:acasereportofsustainedhematologicresponsefollowinganabbreviatedexposure.JHematolOncol.2010Apr23;3:16.doi:10.1186/1756-8722-3-16.PubMedPMID:20416051;PubMedCentralPMCID:PMC2873355.6:SteensmaDP.Noveltherapiesformyelodysplasticsyndromes.HematolOncolClinNorthAm.2010Apr;24(2):423-41.doi:10.1016/j.hoc.2010.02.010.Review.PubMedPMID:20359635.7:D'AlòF,GrecoM,CriscuoloM,VosoMT.Newtreatmentsformyelodysplasticsyndromes.MediterrJHematolInfectDis.2010Aug11;2(2):e2010021.doi:10.4084/MJHID.2010.021.PubMedPMID:21415972;PubMedCentralPMCID:PMC3033133.8:RazaA,GaliliN,CallanderN,OchoaL,PiroL,EmanuelP,WilliamsS,BurrisH3rd,FaderlS,EstrovZ,CurtinP,LarsonRA,KeckJG,JonesM,MengL,BrownGL.Phase1-2amulticenterdose-escalationstudyofezatiostathydrochlorideliposomesforinjection(Telintra,TLK199),anovelglutathioneanalogprodruginpatientswithmyelodysplasticsyndrome.JHematolOncol.2009May13;2:20.doi:10.1186/1756-8722-2-20.PubMedPMID:19439093;PubMedCentralPMCID:PMC2694211.9:RazaA,GaliliN,SmithS,GodwinJ,LancetJ,MelchertM,JonesM,KeckJG,MengL,BrownGL,ListA.Phase1multicenterdose-escalationstudyofezatiostathydrochloride(TLK199tablets),anovelglutathioneanalogprodrug,inpatientswithmyelodysplasticsyndrome.Blood.2009Jun25;113(26):6533-40.doi:10.1182/blood-2009-01-176032.Epub2009Apr27.PubMedPMID:19398716.