MCE蚂蚁淘在线

Incellularassays,INCB024360(INCB024360)selectivelyinhibitshumanIDO1withIC₅₀valuesofapproximately10nM,demonstratinglittleactivityagainstotherrelatedenzymessuchasIDO2ortryptophan2,3-dioxygenase(TDO).INCB024360alsoexhibitssignificantactivitytowardmouseIDO1,withanIC₅₀valueof52.4nM±15.7nM,inasimilarassayusingmouseIDO1-transfectedHEK293/MSRcells^[1].

InVivo

FemaleBalb/cmicebearingCT26tumorsaretreatedorallytwicedailyfor12dwithINCB024360(INCB024360)at100mg/kg.INCB024360suppresseskynurenineequivalentlyinplasma,tumors,andlymphnodes.InnaïveC57BL/6mice,50mg/kgINCB024360decreasesplasmakynureninelevelswithin1hourandthoselevelsstayatleast50%suppressedthroughthe8-hourtimecourse^[2].

ClinicalTrial

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References

[1].LiuX,etal.SelectiveinhibitionofIDO1effectivelyregulatesmediatorsofantitumorimmunity.Blood.2010Apr29;115(17):3520-30.
[2].KoblishHK,etal.Hydroxyamidineinhibitorsofindoleamine-2,3-dioxygenasepotentlysuppresssystemictryptophancatabolismandthegrowthofIDO-expressingtumors.MolCancerTher.2010Feb;9(2):489-98.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.2819mL	11.4095mL	22.8191mL
5mM	0.4564mL	2.2819mL	4.5638mL
10mM	0.2282mL	1.1410mL	2.2819mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

CellAssay
^[1]

INCB024360(INCB024360)isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse^[1].

TodetermineINCB024360activityagainstIDOinrecombinantcells,HEK293/MSRcellsaretransientlytransfectedwithfull-lengthhumanormouseIDO1,ormouseIDO2CDNA,withTransit-293transfectionreagentorLipofectamine2000reagents.INCB024360atdifferentconcentrationsisaddedtotherecoveredtransfectedcellsseededat2×10⁴cellsperwellina96-wellplate(200μL/well).Thecellsareincubatedfor2days,andkyninthesupernatantsismeasuredasdescribedintheHeLacellassay.Thetryptophan2,3-dioxygenase(TDO)assayisperformedsimilarlywithHEK293/MSRcellstransfectedwithahumanTDOexpressionvector^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
^[2]

INCB024360(INCB024360)ispreparedin40%N,N-Dimethylacetamide,60%propyleneglycol(Mice)^[2].

Mice^[2]
ThefemaleC57BL/6micearedosedorallywith50mg/kgINCB024360.C57BL/6wild-typeorIdo1^-/--deficientmiceareadministeredasingleoraldoseofINCB024360,atwhichpointfoodisremovedfromthecagesuntilafterthe8-htimepoint.Atvarioustimepointsafterdosing,miceareeuthanizedandbloodiscollectedbycardiacpuncture.PlasmaisanalyzedforthepresenceofINCB023843,INCB024360,tryptophan,andkynurenineaccordingtothemethodsbelow.Dataareanalyzedusingone-wayANOVAwithDunnett"sposttestforstatisticalsignificance.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].LiuX,etal.SelectiveinhibitionofIDO1effectivelyregulatesmediatorsofantitumorimmunity.Blood.2010Apr29;115(17):3520-30.
[2].KoblishHK,etal.Hydroxyamidineinhibitorsofindoleamine-2,3-dioxygenasepotentlysuppresssystemictryptophancatabolismandthegrowthofIDO-expressingtumors.MolCancerTher.2010Feb;9(2):489-98.

MolecularWeight

438.23

Formula

C₁₁H₁₃BrFN₇O₄S

CASNo.

1204669-58-8

Storage

Powder	-20°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥31mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.65%

SelectBatch: