Itacitinib-INCB039110-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEItacitinibCat.No.:HY-16997CASNo.:1334298-90-6Synonyms:INCB039110分⼦式:C₂₆H₂₃F₄N₉O分⼦量:553.51作⽤靶点:JAK作⽤通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥30mg/mL(54.20mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8067mL9.0333mL18.0665mL5mM0.3613mL1.8067mL3.6133mL10mM0.1807mL0.9033mL1.8067mL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1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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:≥2.5mg/mL(4.52mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.52mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.52mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Itacitinib(INCB039110)⼀种有效的，选择性的JAK1抑制剂，对⼈JAK1的IC50值为2nM。Itacitinib对JAK1选择性JAK2的20多倍，JAK3和TYK2的100多倍。IC50&TargetJAK1体外研究Itacitinib(INCB039110)isapotentandselectiveinhibitorofJAK1,with>20-foldselectivityforJAK1overJAK2and>100-foldoverJAK3andTYK2.Itacitinibisusedintheresearchofmyelofibrosis[1].户使⽤本产品发表的科研⽂献•JAutoimmun.2019May;99:39-47.•Leukemia.2019Aug;33(8):1964-1977.•JCIInsight.2021Apr8;6(7):142205.•EMBORep.2019Jun;20(6):e47202.•EMBORep.2019Jun;20(6):e47202.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MascarenhasJO,etal.PrimaryanalysisofaphaseIIopen-labeltrialofINCB039110,aselectiveJAK1inhibitor,inpatientswithmyelofibrosis.Haematologica.2017Feb;102(2):327-335.[2].AlainLescoat,etal.CombinedAnti-FibroticandAnti-InflammatoryPropertiesofJAK-inhibitorsonMacrophagesinVitroandinVivo:PerspectivesforScleroderma-AssociatedInterstitialLungDisease.BiochemPharmacol.2020Jun17;114103.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc