Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELinrodostatCat.No.:HY-101560CASNo.:1923833-60-6Synonyms:BMS-986205;ONO-7701分?式:C??H??ClFN?O分?量:410.91作?靶點:Indoleamine2,3-Dioxygenase(IDO)作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(121.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4336mL12.1681mL24.3362mL5mM0.4867mL2.4336mL4.8672mL10mM0.2434mL1.2168mL2.4336mL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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(5.06mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.06mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.06mM);Clearsolution4.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:2.5mg/mL(6.08mM);Suspendedsolution;Needultrasonic5.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(6.08mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Linrodostat(BMS-986205)?種選擇性的不可逆的吲哚胺2,3-雙加氧酶1(IDO1)抑制劑，對IDO1-HEK293細(xì)胞具有有效的抑制作?，其IC50值為1.1nM。Linrodostat在晚期癌癥中具有良好的藥理活性。IC50&TargetIDO11.1nM(IC50)體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻?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?邊的抑制劑?師www.MedChemE30820.[2].LillianL.Siu,etal.AbstractCT116:BMS-986205,anoptimizedindoleamine2,3-dioxygenase1(IDO1)inhibitor,iswelltoleratedwithpotentpharmacodynamic(PD)activity,aloneandincombinationwithnivolumab(nivo)inadvancedcancersinaphase1/2aMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical