BMS-1-PD-1-PD-L1-inhibitor-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBMS-1Cat.No.:HY-19991CASNo.:1675201-83-8Synonyms:PD-1/PD-L1inhibitor1分?式:C??H??NO?分?量:475.58作?靶點(diǎn):PD-1/PD-L1;Apoptosis作?通路:Immunology/Inflammation;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)Methanol:25mg/mL(52.57mM;Needultrasonic)DMSO:9mg/mL(18.92mM;Needultrasonicandwarming)DMF:5mg/mL(10.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1027mL10.5135mL21.0270mL5mM0.4205mL2.1027mL4.2054mL10mM0.2103mL1.0513mL2.1027mL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。-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1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、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(2.10mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(2.10mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1mg/mL(2.10mM);ClearsolutionBIOLOGICALACTIVITY?物活性BMS-1PD-1/PD-L1蛋?質(zhì)/蛋?質(zhì)相互作?的抑制劑，IC50為6到100nM[1][2]。IC50&TargetPD1-PDL1[1]體外研究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.體內(nèi)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.戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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