Tretazicar-CB-1954-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETretazicarCat.No.:HY-13543CASNo.:21919-05-1Synonyms:CB1954分⼦式:C₉H₈N₄O₅分⼦量:252.18作⽤靶点:DNAAlkylator/Crosslinker作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(495.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.9654mL19.8271mL39.6542mL5mM0.7931mL3.9654mL7.9308mL10mM0.3965mL1.9827mL3.9654mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.25mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(8.25mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Tretazicar(CB1954)⼀种抗肿瘤前药，对Walker256⼤⿏肿瘤细胞系具有很⾼的效⼒和选择性。Tretazicar酶促活化后⽣成双功能试剂，该试剂可以形成DNA-DNA链间交联。⼤⿏细胞中的Tretazicar涉及通过酶NAD(P)H：醌氧化还原酶1(NQO1)将其4-硝还原为4-羟胺。体外研究Tretazicar(CB1954)(0.1-1000μM;3days)hassensitivityforretrovirallytransducedAB22(AB22-nr)cellswithanIC50of3μM[3].DNAcross-linkformationinaffectedcellsisaresultofthebioactivationofthedrugbytheenzymeDTdiaphorase(NAD(P)Hdehydro-genase(quinone))intheWalkercellswhichreducesthe4-nitrogroupofTretazicar.Theproductofthisreactionisadifunctionalalkylatingagent,5-aziridin-1-yl-4-hydroxylamino-2-nitrobenzamide[4].体内研究Tretazicar(CB1954)(80mg/kg;i.p.ondays2and9)resultsinasignificantincreaseinsurvival[3].AnimalModel:FemaleBALB/cmice(AB22-nr,SKOV3humanovariantumourxenograft)[3]Dosage:80mg/kgAdministration:i.p.ondays2and9Result:ThemediansurvivaloftheAB22-nrwas49days.Resultedinasignificantincreaseinsurvival.REFERENCES[1].KnoxRJ,etal.Bioactivationof5-(aziridin-1-yl)-2,4-dinitrobenzamide(CB1954)byhumanNAD(P)Hquinoneoxidoreductase2:anovelco-substrate-mediatedantitumorprodrugtherapy.CancerRes.2000Aug1;60(15):4179-86.[2].KnoxRJ,etal.CB1954:fromtheWalkertumortoNQO2andVDEPT.CurrPharmDes.2003;9(26):2091-104.[3].GreenNK,etal.Immuneenhancementofnitroreductase-inducedcytotoxicity:studiesusingabicistronicadenovirusvector.IntJCancer.2003Mar10;104(1):104-12.[4].DrabekD,etal.TheexpressionofbacterialnitroreductaseintransgenicmiceresultsinspecificcellkillingbytheprodrugCB1954.GeneTher.1997Feb;4(2):93-100.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala