Deucravacitinib-BMS-986165-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDeucravacitinibCat.No.:HY-117287CASNo.:1609392-27-9Synonyms:BMS-986165分⼦式:C₂₀H₁₉D₃N₈O₃分⼦量:425.46作⽤靶点:JAK;InterleukinRelated;IFNAR作⽤通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt;Immunology/Inflammation储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:37.5mg/mL(88.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3504mL11.7520mL23.5040mL5mM0.4701mL2.3504mL4.7008mL10mM0.2350mL1.1752mL2.3504mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.89mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.89mM);Clearsolution3.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:3.83mg/mL(9.00mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Deucravacitinib(BMS-986165)⼀种⾼效选择性的，⼝服⽣物可利⽤的TYK2变构抑制剂，有潜⼒⽤于⾃⾝免疫性疾病的研究，Deucravacitinib选择性结合TYK2假激酶(JH2)结构域(IC50=1.0nM)，并通过稳定调节JH2结构域来阻断受体介导的Tyk2激活。Deucravacitinib抑制IL-12/23和I型IFN途径[1][2]。IC50&TargetTyk2JH2JAK1JH2IL-12IL-230.2nM(IC50)1nM(IC50)体外研究Deucravacitinib(BMS-986165)isdifferentiatedfrompreviousJAKinhibitorsdueitsuniqueabilitytoselectivelybindtothepseudokinase(JH2)domainofTYK2andinhibititsfunctionthroughanallostericmechanism[1].Deucravacitinibmaintainsexcellentpotencyinhumanandmousewholeblood(IC50s=13and100nM,respectively)andshowsnosignificanthERGinhibitioninthefluxassay(IC50>80μM)[1].户使⽤本产品发表的科研⽂献•NatChemBiol.2022Sep12.•CellDeathDiffer.2021Feb;28(2):748-763.•IntJMolSci.2022May1;23(9):5040.•iScience.2021,102498.•ArthritisResTher.2021Apr19;23(1):120.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WrobleskiST,etal.HighlySelectiveInhibitionofTyrosineKinase2(TYK2)fortheTreatmentofAutoimmuneDiseases:DiscoveryoftheAllostericInhibitorBMS-986165.JMedChem.2019Jul18.[2].CatlettI,etal.SAT0226Afirst-in-human,studyofBMS-986165,aselective,potent,allostericsmallmoleculeinhibitoroftyrosinekinase2.AnnalsoftheRheumaticDiseases2017;76:859.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica