V-9302-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEV-9302Cat.No.:HY-112683CASNo.:1855871-76-9分⼦式:C₃₄H₃₈N₂O₄分⼦量:538.68作⽤靶点:Others作⽤通路:Others储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:25mg/mL(46.41mM;ultrasonicandwarmingandheatto80°C)H2O:<0.1mg/mL(ultrasonic)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8564mL9.2819mL18.5639mL5mM0.3713mL1.8564mL3.7128mL10mM0.1856mL0.9282mL1.8564mL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(sealedstorage,awayfrommoisture)。-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:≥1mg/mL(1.86mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:1mg/mL(1.86mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1mg/mL(1.86mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性V-9302跨膜⾕氨酰胺通量的竞争性拮抗剂。V-9302有效选择性的靶向氨酸转运体ASCT2(SLC1A5)，不ASCT1。V-9302抑制了HEK-293细胞中由ASCT2介导的⾕氨酰胺摄取(IC50=9.6μM)[1]。IC50&TargetASCT2[1]体外研究V-9302inhibitsASCT2-mediatedglutamineuptakeinhumancellsinaconcentration-dependentfashionandexhibitsa100-foldimprovementinpotencyovergamma-L-glutamyl-p-nitroanilide[1].PharmacologicalblockadeofASCT2withV-9302resultsinattenuatedcancercellgrowthandproliferation,increasescelldeath,andincreasesoxidativestress[1].体内研究V-9302(75mg/kg;i.p.;dailyfo21days)preventstumorgrowthinbothHCT-116andHT29xenograftmodels[1].ThecombinationofCB-839andV-9302(30mg/kg;i.p.;SNU398andMHCC97HcellsweregrownastumorxenograftsinBALB/cnudemice;for20or15d,respectively)elicitsastronggrowthinhibitioninbothSNU398andMHCC97Hxenograftmodels,whilesingle-drugtreatmentshowedmodestanti-tumoreffects[2].V-9302(50mg/kg;i.p.;dailyfor5days)displaysmarkedlyreducedtumorgrowth[3].AnimalModel:6-weekold,femaleathymicnudemice(bearingHCT-116(KRASG13D)orHT29(BRAFV600E)cell-line)[1]Dosage:75mg/kgAdministration:Intraperitoneally;dailyfo21daysResult:Preventedtumorgrowth.户使⽤本产品发表的科研⽂献•CellMetab.2022Nov11;S1550-4131(22)00490-9.•JNanobiotechnology.2022May6;20(1):216.•FrontPharmacol.2021May14;12:671328.•JBiolChem.2022Feb18;101753.•MagnResonImaging.2022Aug24;S0730-725X(22)00149-7.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].SchulteML,etal.PharmacologicalblockadeofASCT2-dependentglutaminetransportleadstoantitumorefficacyinpreclinicalmodels.NatMed.2018Feb;24(2):194-202.[2].JinH,etal.Apowerfuldrugcombinationstrategytargetingglutamineaddictionforthetreatmentofhumanlivercancer.Elife.2020;9:e56749.Published2020Oct5.[3].EdwardsDN,etal.SelectiveglutaminemetabolisminhibitionintumorcellsimprovesantitumorTlymphocyteactivityintriple-negativebreastcancer.JClinInvest.2021;131(4):e140100.McePdfHeightCaution:Producthasnotb