GDC-0879isanorallybioavailablekinaseinhibitorthatexhibitsanticancerchemotherapeuticactivityinvitroandinvivo.GDC-0879inhibitsmutant(V600E)B-Raf,amutationcommontomanytypesofcancer.ThisinhibitionofmutantB-RafdecreasesMEK1phosphorylation,downregulatingexpressionofgenesassociatedwithcellproliferationandresultinginsustainedinhibitionoftumorcellproliferation.
| CasNo. | 905281-76-7 |
|---|---|
| Purity | ≥96% |
| Formula | C19H18N4O2 |
| FormulaWt. | 334.37 |
| ChemicalName | (E)-5-(1-(2-hydroxyethyl)-3-(pyridin-4-yl)-1H-pyrazol-4-yl)-2,3-dihydroinden-1-oneoxime |
| IUPACName | 2-[4-[(1E)-1-hydroxyimino-2,3-dihydroinden-5-yl]-3-pyridin-4-ylpyrazol-1-yl]ethanol |
| Solubility | DMSO67mg/mL |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| MSDS | G1208MSDSPDF |
|---|---|
| InfoSheet | G1208InfoSheetPDF |
| Brochures | Ras-Raf-MEK-ERKPathwayBooklet |
HoeflichKP,HerterS,TienJ,etal.AntitumorefficacyofthenovelRAFinhibitorGDC-0879ispredictedbyBRAFV600Emutationalstatusandsustainedextracellularsignal-regulatedkinase/mitogen-activatedproteinkinasepathwaysuppression.CancerRes.2009Apr1;69(7):3042-51.PMID:19276360.
WongH,BelvinM,HerterS,etal.Pharmacodynamicsof2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol(GDC-0879),apotentandselectiveB-Rafkinaseinhibitor:understandingrelationshipsbetweensystemicconcentrations,phosphorylatedmitogen-activatedproteinkinasekinase1inhibition,andefficacy.JPharmacolExpTher.2009Apr;329(1):360-7.PMID:19147858.
