MedKoo Biosciences/Ezatiostat/201360/5mg

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¥3000.00
货号:201360-5mg
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品牌:MedKoo
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商品描述
EzatiostatisaLiposomalsmall-moleculeglutathioneanaloginhibitorofglutathioneS-transferase(GST)P1-1withhematopoiesis-stimulatingactivity.Afterintracellularde-esterification,theactiveformofezatiostatbindstoandinhibitsGSTP1-1,therebyrestoringJunkinaseandMAPKpathwayactivitiesandpromotingMAPK-mediatedcellularproliferationanddifferentiationpathways.Thisagentpromotestheproliferationandmaturationofhematopoieticprecursorcells,granulocytes,monocytes,erythrocytesandplatelets.Checkforactiveclinicaltrialsorclosedclinicaltrialsusingthisagent.(NCIThesaurus).

MedKooCat#:201360
Name:Ezatiostat
CAS#:168682-53-9(freebase)
ChemicalFormula:C27H35N3O6S
ExactMass:529.22466
MolecularWeight:529.6483
ElementalAnalysis:C,61.23;H,6.66;N,7.93;O,18.12;S,6.05


Synonym:TLK199;TLK-199;TLK199;Ezatiostat;Brandname:TELINTRA

IUPAC/ChemicalName:(S)-ethyl2-amino-5-(((R)-3-(benzylthio)-1-(((S)-2-ethoxy-2-oxo-1-phenylethyl)amino)-1-oxopropan-2-yl)amino)-5-oxopentanoate

InChiKey:GWEJFLVSOGNLSS-FIXSFTCYSA-N

InChiCode: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/s1

SMILESCode: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)=O


TechnicalData

Appearance:
Whitesolidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

CertificateofAnalysis:
ViewCoA,currentbatch,Lot#CRB40225

QCData:
ViewQCdata:currentbatch,Lot#CRB40225.

SafetyDataSheet(MSDS):
ViewMaterialSafetyDataSheet(MSDS)

ShippingCondition:
Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:
Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:
SolubleinDMSO,notinwater

ShelfLife:
>2yearsifstoredproperly

DrugFormulation:
ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:
0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:
293490


AdditionalInformation

RelatedCAS#
168682-53-9(Ezatiostat);
286942-97-0(EzatiostatHClsalt)
 


References

1: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.

苏州蚂蚁淘代理MedKoo在中国的业务。 MedKoo北京代理,MedKoo华东代理,MedKoo华北代理,MedKoo华中代理,MedKoo华南代理,MedKoo全国代理。 MedKoo公司是2009年由Qingqi Chen博士创立。在美国北卡罗来纳州的三角研究园区有运营办公室,其研发和生产车间位于中国。陈博士在加入MedKoo之前,是中山大学药学院(中山大学,中国广州)和中国科学院(北京)“100人计划”的杰出教授。对小分子抗癌药物有浓厚兴趣,发表了100多篇论文,获得20多项。Medkoo是处于先进地位的小分子抗癌试剂,激酶抑制剂和其他相关化学品的优秀供应商。 MedKoo部分产品列表:MedKoo全国代理 406757 10058-F4 530576 10074-G5 600110 10-Deacetylbaccatin III 530429 10-Gingerol 406281 10-Hydroxycamptothecin 341231 10-Hydroxyyohimbine 571387 [11C]-ABP688 526406 11-deoxy-PGF2a 525629 123C4   561223 12-Crown-4 featured 525697 1,3,5,6-Tetrahydroxyxanthone 526087 1,3,5-Trihydroxyxanthone 584120 1,3,7-Trimethyluric acid 527871 1,3-Dicaffeoylquinic acid 530605 1400W HCl