Vipivotide-tetraxetan-PSMA-617-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVipivotidetetraxetanCat.No.:HY-117410CASNo.:1702967-37-0Synonyms:PSMA-617分⼦式:C₄₉H₇₁N₉O₁₆分⼦量:1042.14作⽤靶点:Drug-LinkerConjugatesforADC作⽤通路:Antibody-drugConjugate/ADCRelated储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(119.95mM;Needultrasonic)H2O:≥100mg/mL(95.96mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM0.9596mL4.7978mL9.5956mL5mM0.1919mL0.9596mL1.9191mL10mM0.0960mL0.4798mL0.9596mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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(2.00mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(2.00mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(2.00mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Vipivotidetetraxetan(PSMA-617)前列腺特异性膜抗原(PSMA)的强有效抑制剂，其Ki值为0.37nM。Vipivotidetetraxetan(PSMA-617)由三种成分组成:药效团Glutamate-urea-Lysine，螯合剂DOTA（能够结合68Ga或177Lu），以及连接这两个实体的linker。Glutamate-urea-Lysine可以与前列腺特异性膜抗原(PSMA)选择性结合。IC50&TargetTraditionalCytotoxicAgents体外研究Vipivotidetetraxetan(PSMA-617)demonstrateshighradiolyticstabilityforatleast72h.Ahighinhibitionpotency(equilibriumdissociationconstantKi=2.34±2.94nMonLNCaP;Ki=0.37±0.21nMenzymaticallydetermined)andhighlyefficientinternalizationintoLNCaPcellsaredemonstrated[1].体内研究Organdistributionwith68Ga-labeledVipivotidetetraxetan(PSMA-617)after1h(n=3)revealsahighspecificuptakeinLNCaPtumorsandinthekidneys.Thehighuptakeinthekidneysisnearlycompletelyblockedbycoinjectionof2mgof2-PMPAperkilogram.Otherorganssuchastheliver,lung,andspleenshowratherlowuptakeandnoblockingeffect,withtheexceptionofthespleen.Tumor-to-backgroundratiosare7.8(tumortoblood)and17.1(tumortomuscle)at1hafterinjection.Ascomparedwiththe68Ga-labeledversion,theorgandistributionwith177Lu-labeledVipivotidetetraxetan(PSMA-617)(n=3)showasimilaruptakeintheLNCaPtumorsandinthekidneys.Theliveruptakeisfoundtobestatisticallydifferent.Tumor-to-backgroundratiosdetermined1hafterinjectionshowslightlyhighervalues(tumortoblood,22.1;tumortomuscle,25.6)thanpreviousorgandistributionwith68Ga-labeledVipivotidetetraxetan(PSMA-617)[1].户使⽤本产品发表的科研⽂献•Pharmaceutics.2022Mar28;14(4):731.•Biomolecules.2021Feb10;11(2):263.•MolPharm.2022Jul27.•Pharmaceuticals.2022Sep19;15(9):1161.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].BenešováM,etal.PreclinicalEvaluationofaTailor-MadeDOTA-ConjugatedPSMAInhibitorwithOptimizedLinkerMoietyforImagingandEndoradiotherapyofProstateCancer.JNuclMed.2015Jun;56(6):914-20.McePdfHeightCaution:Producthasnotbeenf