Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPD-1/PD-L1-IN-9Cat.No.:HY-132192CASNo.:2628506-54-5分?式:C??H??N?O?分?量:348.44作?靶點:PD-1/PD-L1作?通路:Immunology/Inflammation儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(286.99mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8699mL14.3497mL28.6993mL5mM0.5740mL2.8699mL5.7399mL10mM0.2870mL1.4350mL2.8699mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.17mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.17mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.17mM);ClearsolutionBIOLOGICALACTIVITY?物活性PD-1/PD-L1-IN-9?種有效和具有?服活性的PD-1/PD-L1相互作?抑制劑，IC50值為3.8nM。PD-1/PD-L1-IN-9可以增強(qiáng)免疫細(xì)胞對腫瘤細(xì)胞的殺傷活性。PD-1/PD-L1-IN-9在CT26??模型中表現(xiàn)出顯的體內(nèi)抗腫瘤活性。IC50&TargetIC50:3.8nM(PD-1/PD-L1)[1]體外研究PD-1/PD-L1-IN-9(compound24)(46.9-1500nM;pretreatedfor2h)dose-dependentlysignificantlyactivatestheantitumorimmunityofPBMCstoMDB-MB231cells,withanEC50of-100nM[1].體內(nèi)研究PD-1/PD-L1-IN-9(compound24)(40-80mg/kg;p.o.onceadayfor2weeks)inhibitstumorgrowthinadose-dependentmanneranddoesnotcauseanybodyweightlossormortalityofmice[1].PD-1/PD-L1-IN-9(3mg/kg;asinglei.v.)exhibitshalf-life(t1/2=4.2h),plasmaclearance(Cl=11.5L/h/kg)andCmax(1233ng/mL)inrats[1].PD-1/PD-L1-IN-9(25mg/kg;asinglep.o.)exhibitsmoderateoralbioavailability(F=22%),half-life(t1/2=6.4h)andCmax(192ng/mL)inrats[1].AnimalModel:MaleBALB/cmice(5-6weeks)wereinoculatedCT26cells[1]Dosage:40,80mg/kgAdministration:P.o.onceadayfor2weeksResult:Significantlydecreasedthefinaltumorweight,withTGIvaluesof60and67%atthedoseof40and80mg/kg,respectively.AnimalModel:Sprague-Dawley(SD)rats[1]Dosage:3mg/kgfori.v.and25mg/kgforp.o.(PharmacokineticAnalysis)Administration:Asinglei.v.orp.o.Result:I.v.:t1/2=4.2h;Cl=11.5L/h/kg;Cmax=1233ng/mL.P.o.:F=22%;t1/2=6.4h;Cmax=192ng/mL.REFERENCES[1].WangT,et,al.NovelBiphenylPyridinesasPotentSmall-MoleculeInhibitorsTargetingtheProgrammedCellDeath-1/ProgrammedCell2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDeath-Ligand1Interaction.JMedChem.2021May30.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical