Deucravacitinib-BMS-986165-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDeucravacitinibCat.No.:HY-117287CASNo.:1609392-27-9Synonyms:BMS-986165分?式:C??H??D?N?O?分?量:425.46作?靶點:JAK;InterleukinRelated;IFNAR作?通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt;Immunology/Inflammation儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:37.5mg/mL(88.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3504mL11.7520mL23.5040mL5mM0.4701mL2.3504mL4.7008mL10mM0.2350mL1.1752mL2.3504mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.89mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.89mM);Clearsolution3.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:3.83mg/mL(9.00mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Deucravacitinib(BMS-986165)?種?效選擇性的，?服?物可利?的TYK2變構(gòu)抑制劑，有潛??于??免疫性疾病的研究，Deucravacitinib選擇性結(jié)合TYK2假激酶(JH2)結(jié)構(gòu)域(IC50=1.0nM)，并通過穩(wěn)定調(diào)節(jié)JH2結(jié)構(gòu)域來阻斷受體介導的Tyk2激活。Deucravacitinib抑制IL-12/23和I型IFN途徑[1][2]。IC50&TargetTyk2JH2JAK1JH2IL-12IL-230.2nM(IC50)1nM(IC50)體外研究Deucravacitinib(BMS-986165)isdifferentiatedfrompreviousJAKinhibitorsdueitsuniqueabilitytoselectivelybindtothepseudokinase(JH2)domainofTYK2andinhibititsfunctionthroughanallostericmechanism[1].Deucravacitinibmaintainsexcellentpotencyinhumanandmousewholeblood(IC50s=13and100nM,respectively)andshowsnosignificanthERGinhibitioninthefluxassay(IC50>80μM)[1].戶使?本產(chǎn)品發(fā)表的科研?獻?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