Doramapimodisananticancerchemotherapeuticinhibitorofp38MAPKandJNKthatalsodisplayssomeinvitroactivityagainstanaplasticlymphomakinase(ALK).Doramapimodiscurrentlyinclinicaltrialsasapotentialtreatmentforinflammatorydiseases,exhibitinganti-inflammatoryactivity.Invitro,thiscompoundinhibitsexpressionofCOX-2,MMP13,iNOS,andTNF-αanddecreasesreleaseofprostaglandinE2(PGE2),decreasingtheoverallinflammatoryresponse.
| CasNo. | 2859873-48-4 |
|---|---|
| Purity | ≥98% |
| Formula | C31H37N5O3 |
| FormulaWt. | 527.66 |
| ChemicalName | 1-(3-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl)-3-(4-(2-(morpholin-4-yl)ethoxy)naphthalen-1-yl)urea |
| IUPACName | 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea |
| Synonym | 1-[2-(4-Methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea;BIRB796 |
| Appearance | Whitetooffwhitepowder |
| StoreTemp | Ambient |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | D5868InfoSheetPDF |
|---|
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afGennäsGB,MologniL,AhmedS,etal.Design,synthesis,andbiologicalactivityofureaderivativesasanaplasticlymphomakinaseinhibitors.ChemMedChem.2011Sep5;6(9):1680-92.PMID:21721129.
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JoosH,AlbrechtW,LauferS,etal.Differentialeffectsofp38MAPkinaseinhibitorsontheexpressionofinflammation-associatedgenesinprimary,interleukin-1beta-stimulatedhumanchondrocytes.BrJPharmacol.2010Jul;160(5):1252-62.PMID:20590617.
GruenbaumLM,SchwartzR,WoskaJRJr,etal.Inhibitionofpro-inflammatorycytokineproductionbythedualp38/JNK2inhibitorBIRB796correlateswiththeinhibitionofp38signaling.BiochemPharmacol.2009Feb1;77(3):422-32.PMID:19027720.
KumaY,SABIoG,BainJ,etal.BIRB796inhibitsallp38MAPKisoformsinvitroandinvivo.JBiolChem.2005May20;280(20):19472-9.PMID:15755732.
