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MedKoo Biosciences/Ethaselen/206121/1g

Ethaselen,alsoknownasBBSKE,isanovelorganoseleniumthioredoxinreductaseinhibitor,iscurrentlybeinginvestigatedinaphaseIclinicaltrialinChina.Ethaselenenhancedtheefficacyofradiationtherapybothinvivoandinvitrowithoutobservabletoxicity.BBSKEwasfoundtosuppressirradiation-inducedNF-κBactivationdramaticallywhenusingA549cellsstablytransfectedwithNF-κBluciferasereporter.EthaselenisapotentiallypromisingagentforthetreatmentofpatientswithNSCLCclinically.

MedKooCat#:206121
Name:Ethaselen
CAS#:217798-39-5
ChemicalFormula:C16H12N2O2Se2
ExactMass:423.92292
MolecularWeight:422.2
ElementalAnalysis:C,45.52;H,2.86;N,6.64;O,7.58;Se,37.40


Synonym:Ethaselen;12bis(12benzisoselenazolone3(2H)ketone)ethaneBBSKE.

IUPAC/ChemicalName:2,2-(ethane-1,2-diyl)bis(benzo[d][1,2]selenazol-3(2H)-one).

InChiKey:SFFSGPCYJCMDJM-UHFFFAOYSA-N

InChiCode:InChI=1S/C16H12N2O2Se2/c19-15-11-5-1-3-7-13(11)21-17(15)9-10-18-16(20)12-6-2-4-8-14(12)22-18/h1-8H,9-10H2

SMILESCode:O=C1N(CCN2[Se]C3=CC=CC=C3C2=O)[Se]C4=CC=CC=C14


TechnicalData

Appearance:
whitesolidpowder

Purity:
>98%(orrefertotheCertificateofAnalysis)

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

  
 
 
 


References

1:WangL,YangZ,FuJ,YinH,XiongK,TanQ,JinH,LiJ,WangT,TangW,YinJ,CaiG,LiuM,KehrS,BeckerK,ZengH.Ethaselen:apotentmammalianthioredoxinreductase1inhibitorandnovelorganoseleniumanticanceragent.FreeRadicBiolMed.2012Mar1;52(5):898-908.doi:10.1016/j.freeradbiomed.2011.11.034.Epub2011Dec21.PubMedPMID:22210352.

2:WangL,FuJN,WangJY,JinCJ,RenXY,TanQ,LiJ,YinHW,XiongK,WangTY,LiuXM,ZengHH.Selenium-containingthioredoxinreductaseinhibitorethaselensensitizesnon-smallcelllungcancertoradiotherapy.AnticancerDrugs.2011Sep;22(8):732-40.doi:10.1097/CAD.0b013e32834618bc.PubMedPMID:21562407.

3:ZhouHY,MengZY,DouGF,MaJL,LouYQ,ZhangGL.[LC-MSnanalysisofmetabolitesof1,2-[bis(1,2-benzisoselenazolone-3(2H)-ketone)]-ethane,anovelanti-canceragentinrat].YaoXueXueBao.2010May;45(5):627-31.Chinese.PubMedPMID:20931766.

4:YinH,LiJ,XiongK,WangL,WangT,TanQ,FuJ,RenX,ZengH.NovelmechanismofethaseleninpoorlydifferentiatedcolorectalRKOcellgrowthinhibition:SimultaneousregulationofTrxRtranscription,expressionandenzymeactivity.Differentiation.2011Jan;81(1):49-56.doi:10.1016/j.diff.2010.09.180.PubMedPMID:20864247.

5:LiuM,FuJ,LiJ,WangL,TanQ,RenX,PengZ,ZengH.Preparationoftri-blockcopolymermicellesloadingnovelorganoseleniumanticancerdrugBBSKEandstudyoftissuedistributionofcopolymermicellesbyimaginginvivomethod.IntJPharm.2010May31;391(1-2):292-304.doi:10.1016/j.ijpharm.2010.03.001.Epub2010Mar6.PubMedPMID:20211232.

6:FuJN,LiJ,TanQ,YinHW,XiongK,WangTY,RenXY,ZengHH.ThioredoxinreductaseinhibitorethaselenincreasesthedrugsensitivityofthecoloncancercelllineLoVotowardscisplatinviaregulationofG1phaseandreversalofG2/Mphasearrest.InvestNewDrugs.2011Aug;29(4):627-36.doi:10.1007/s10637-010-9401-y.Epub2010Mar2.PubMedPMID:20195699.

7:TanQ,RenXY,LiJ,WangF,DengSJ,ZengHH.[CorrelationofplasmathioredoxinreductaseactivitytogrowthofH22hepatocellularcarcinomaxenograftsinKunmingmice].AiZheng.2009May;28(5):472-7.Chinese.PubMedPMID:19624873.

8:TanQ,LiJ,YinHW,WangLH,TangWC,ZhaoF,LiuXM,ZengHH.AugmentedantitumoreffectsofcombinationtherapyofcisplatinwithethaselenasanovelthioredoxinreductaseinhibitoronhumanA549cellinvivo.InvestNewDrugs.2010Jun;28(3):205-15.doi:10.1007/s10637-009-9235-7.Epub2009Mar7.PubMedPMID:19271154.

9:LiX,YangZ,YangK,ZhouY,ChenX,ZhangY,WangF,LiuY,RenL.Self-assembledpolymericmicellarnanoparticlesasnanocarriersforpoorlysolubleanticancerdrugethaselen.NanoscaleResLett.2009Sep16;4(12):1502-11.doi:10.1007/s11671-009-9427-2.PubMedPMID:20652138;PubMedCentralPMCID:PMC2893964.

10:ZhouHY,DouGF,MengZY,LouYQ,ZhangGL.Developmentofarapidandsensitiveliquidchromatography/tandemmassspectrometrymethodforthedeterminationof1,2-[bis(1,2-benzisoselenazolone-3(2H)-ketone)]-ethane(BBSKE),anovelanti-canceragentinratplasma.BiomedChromatogr.2008Oct;22(10):1123-9.doi:10.1002/bmc.1034.PubMedPMID:18651605.


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