Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEV-9302Cat.No.:HY-112683CASNo.:1855871-76-9分?式:C??H??N?O?分?量:538.68作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(46.41mM;ultrasonicandwarmingandheatto80°C)H2O:<0.1mg/mL(ultrasonic)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8564mL9.2819mL18.5639mL5mM0.3713mL1.8564mL3.7128mL10mM0.1856mL0.9282mL1.8564mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1mg/mL(1.86mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:1mg/mL(1.86mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1mg/mL(1.86mM);ClearsolutionBIOLOGICALACTIVITY?物活性V-9302跨膜?氨酰胺通量的競(jìng)爭(zhēng)性拮抗劑。V-9302有效選擇性的靶向氨酸轉(zhuǎn)運(yùn)體ASCT2(SLC1A5)，不ASCT1。V-9302抑制了HEK-293細(xì)胞中由ASCT2介導(dǎo)的?氨酰胺攝取(IC50=9.6μM)[1]。IC50&TargetASCT2[1]體外研究V-9302inhibitsASCT2-mediatedglutamineuptakeinhumancellsinaconcentration-dependentfashionandexhibitsa100-foldimprovementinpotencyovergamma-L-glutamyl-p-nitroanilide[1].PharmacologicalblockadeofASCT2withV-9302resultsinattenuatedcancercellgrowthandproliferation,increasescelldeath,andincreasesoxidativestress[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師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