BMS-1166-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBMS-1166Cat.No.:HY-102011CASNo.:1818314-88-3分⼦式:C₃₆H₃₃ClN₂O₇分⼦量:641.11作⽤靶点:PD-1/PD-L1作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(194.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5598mL7.7990mL15.5979mL5mM0.3120mL1.5598mL3.1196mL10mM0.1560mL0.7799mL1.5598mL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、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:≥2.08mg/mL(3.24mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.24mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性BMS-1166⼀种有效的PD-1/PD-L1免疫检查点抑制剂。BMS-1166诱导PD-L1⼆聚化并阻断其与PD-1的相互作⽤，IC50为1.4nM。BMS-1166拮抗PD-1/PD-L1免疫检查点对T细胞活化的抑制作⽤。IC50&TargetIC50:1.4nM(PD-1/PD-L1interaction)[1].体外研究BMS-1166isapotentPD-1/PD-L1interactioninhibitorwithanIC50of1.4nMinahomogenoustime-resolvedfluorescencebindingassay[1].BMS-1166antagonizestheinhibitoryeffectofPD-1/PD-L1immunecheckpointonTcellactivation.BMS-1166dosedependentlyabolishestheinhibitionofECsstimulationbysPD-L1[2].REFERENCES[1].GuzikK,etal.Small-MoleculeInhibitorsoftheProgrammedCellDeath-1/ProgrammedDeath-Ligand1(PD-1/PD-L1)InteractionviaTransientlyInducedProteinStatesandDimerizationofPD-L1.JMedChem.2017Jul13;60(13):5857-5867.[2].SkalniakL,etal.Small-moleculeinhibitorsofPD-1/PD-L1immunecheckpointalleviatethePD-L1-inducedexhaustionofT-cells.Oncotarget.2017Aug7;8(42):72167-72181.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.