BMS-1-PD-1-PD-L1-inhibitor-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBMS-1Cat.No.:HY-19991CASNo.:1675201-83-8Synonyms:PD-1/PD-L1inhibitor1分⼦式:C₂₉H₃₃NO₅分⼦量:475.58作⽤靶点:PD-1/PD-L1;Apoptosis作⽤通路:Immunology/Inflammation;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验Methanol:25mg/mL(52.57mM;Needultrasonic)DMSO:9mg/mL(18.92mM;Needultrasonicandwarming)DMF:5mg/mL(10.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1027mL10.5135mL21.0270mL5mM0.4205mL2.1027mL4.2054mL10mM0.2103mL1.0513mL2.1027mL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:≥1mg/mL(2.10mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(2.10mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1mg/mL(2.10mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BMS-1PD-1/PD-L1蛋⽩质/蛋⽩质相互作⽤的抑制剂，IC50为6到100nM[1][2]。IC50&TargetPD1-PDL1[1]体外研究SincePD-1mediatedtheexhaustionofnaturalkiller(NK)cellbybindingtoitsligandPD-L1,BMS-1(PD-1/PD-L1inhibitor1)(1μM,3days)isusedtodisturbtheinteractionbetweenPD-1andPD-L1.DexamethasoneinducedincreaseofPD-1expressionanddecreaseofcytotoxicityoftheco-culturedNK92cellsarereversedbyBMS-1[1].BMS-1,asmall-moleculeimmunecheckpointinhibitorofPD-1/PD-L1,canbeusedasatherapeuticstrategyfortumorimmunotherapy[2].CellCytotoxicityAssay[1]CellLine:NKcellsandHepG2cellsConcentration:1μMIncubationTime:3daysResult:DisturbedtheinteractionbetweenPD-1andPD-L1.体内研究BMS-1(500μg/mL;100μL;i.p.)significantlyincreasesthesurvivalratesofthemVEGF165bgroupandmVEGF165b+MUC1group[3].AnimalModel:BALB/cmicewithEMT6cells[3]Dosage:500μg/mL;100μLAdministration:I.p.Result:IncreasedthesurvivalratesofthemVEGF165bgroupandmVEGF165b+MUC1group.mVEGF165bcombinedwithMUC1resultssignificantretardationofthetumorgrowth.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•AdvFunctMater.2021Mar21.•Small.2022Nov11;e2205694.•JExpClinCancerRes.2022Jan3;41(1):1.•JImmunotherCancer.2020Oct;8(2):e000293.•JColloidInterfaceSci.2022Jan24;614:436-450.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhaoY,etal.DepressionPromotesHepatocellularCarcinomaProgressionthroughaGlucocorticoidsMediatedUp-RegulationofPD-1ExpressioninTumorinfiltratingNKCells.Carcinogenesis.2019Feb4.[2].LiK,etal.Developmentofsmall-moleculeimmunecheckpointinhibitorsofPD-1/PD-L1asanewtherapeuticstrategyfortumourimmunotherapy.JDrugTarget.2019Mar;27(3):244-256.[3].ZhangH,etal.UtilizingVEGF165bmutantasaneffectiveimmunizationadjuncttoaugmentantitumorimmuneresponse.Vaccine.2019Apr3;37(15):2090-2098.[4].MengyuanLi,etal.KALRNmutationspromoteantitumorimmunityandimmunotherapyresponseincancer.JImmunotherCancer.2020Oct;8(2):e000293.McePdfHeightCaution:Producthasnot