Linrodostat-BMS-986205-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELinrodostatCat.No.:HY-101560CASNo.:1923833-60-6Synonyms:BMS-986205;ONO-7701分⼦式:C₂₄H₂₄ClFN₂O分⼦量:410.91作⽤靶点:Indoleamine2,3-Dioxygenase(IDO)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(121.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4336mL12.1681mL24.3362mL5mM0.4867mL2.4336mL4.8672mL10mM0.2434mL1.2168mL2.4336mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(5.06mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.06mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.06mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:2.5mg/mL(6.08mM);Suspendedsolution;Needultrasonic5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.08mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Linrodostat(BMS-986205)⼀种选择性的不可逆的吲哚胺2,3-双加氧酶1(IDO1)抑制剂，对IDO1-HEK293细胞具有有效的抑制作⽤，其IC50值为1.1nM。Linrodostat在晚期癌症中具有良好的药理活性。IC50&TargetIDO11.1nM(IC50)体外研究Linrodostat(0.01-100μM;72hours;SKOV-3andJurkatcloneE6-1cells)treatmentreducesthenumberofviablecellscomparedwiththenon-treatedcontrol.LinrodostatalsoinducescelldeathatmuchlowerconcentrationsanditsIC50is6.3μM[1].CellViabilityAssay[1]CellLine:SKOV-3andJurkatcloneE6-1cellsConcentration:0.01-100μMIncubationTime:72hoursResult:Reducedthenumberofviablecellscomparedwiththenon-treatedcontrolandinducedcelldeathatmuchlowerconcentrations.户使⽤本产品发表的科研⽂献•Immunity.2021Sep28;S1074-7613(21)00390-3.•CellDeathDiffer.2021Feb;28(2):715-729.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RichardsT,etal.CellbasedfunctionalassaysforIDO1inhibitorscreeningandcharacterization.Oncotarget.2018Jul20;9(56):30814-2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE30820.[2].LillianL.Siu,etal.AbstractCT116:BMS-986205,anoptimizedindoleamine2,3-dioxygenase1(IDO1)inhibitor,iswelltoleratedwithpotentpharmacodynamic(PD)activity,aloneandincombinationwithnivolumab(nivo)inadvancedcancersinaphase1/2aMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical