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Tocris/MZ 1/6154/5/5 mg
  • Tocris/MZ 1/6154/5/5 mg

Tocris/MZ 1/6154/5/5 mg

价格: ¥4020.00 市场价: 6700.00
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货号: 6154
品牌: Tocris
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    • Description:(+)-JQ1basedPROTACthatselectivelydegradesBRD4incells
      ChemicalName:(2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
      Purity:≥98%(HPLC)
      BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferences

      BiologicalActivity

      CellpenetrantProteolysisTargetingChimera(PROTAC)compoundbasedon(+)-JQ1(Cat.No.4499)conjugatedtoavonHippel-Lindau(VHL)ligand.RetainshighaffinityforBRD2,BRD3andBRD4bromodomains(Kd=13-60nM)butinducespreferentialdegradationofBRD4overBRD2andBRD3(DC50valuesfordegradationofBRD4are8and23nMinH661andH838cells,respectively).ExhibitspotentcytotoxicityandantiproliferativeeffectsinAMLcelllines(pEC50=7.6inMv4;11cells).NegativecontrolcisMZ1alsoavailable.

      PROTACsarebi-functionalsmallmoleculesthatharnesstheubiquitin/proteasomesystem(UPS)toselectivelyandcatalyticallyremovetargetproteinsfromcells.

      LicensingInformation

      SoldunderlicencefromtheUniversityofDundee

      ExternalPortalInformation

      Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofMZ1isreviewedontheChemicalProbeswebsite.

      TechnicalData

      M.Wt1002.64
      FormulaC49H60ClN9O8S2
      StorageStoreat-20°C
      Purity≥98%(HPLC)
      CASNumber1797406-69-9
      PubChemID122201421
      InChIKeyPTAMRJLIOCHJMQ-PYNGZGNASA-N
      SmilesCC1=C(C2=C(N3C(C)=NN=C3[C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)O)=O)=O)=O)S1)C

      Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.

      AllTocrisproductsareintendedforlaboratoryresearchuseonly.

      SolubilityData

      SolventMaxConc.mg/mLMaxConc.mM
      Solubility
      DMSO100.26100
      ethanol100.26100

      PreparingStockSolutions

      Thefollowingdataisbasedontheproductmolecularweight1002.64.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.

      Concentration/SolventVolume/Mass1mg5mg10mg
      1mM1mL4.99mL9.97mL
      5mM0.2mL1mL1.99mL
      10mM0.1mL0.5mL1mL
      50mM0.02mL0.1mL0.2mL