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GDC 0879
- Soluble in DMSO
- MF: C19H18N4O2
- MW: 334.37
Description
GDC 0879 is a potent and selective BRAF kinase inhibitor with strong activity against BRAF V600E and downstream ERK pathway signaling.
GDC 0879 inhibits MAPK signaling in BRAF-mutant cells but, like several ATP-competitive RAF inhibitors, can paradoxically activate ERK signaling in RAS-active cells with wild-type RAF. This context dependence makes it useful for both oncogenic BRAF and RAF-dimerization research.
Key Features
- Potent BRAF V600E inhibitor
- Suppresses MEK–ERK signaling in BRAF-mutant cells
- Can produce paradoxical ERK activation in wild-type RAF contexts
- Useful for studying RAF inhibitor context dependence
Applications
- BRAF kinase and target-engagement assays
- BRAF V600E cancer-cell models
- RAF dimerization and paradoxical activation studies
- MAPK pathway resistance research
More Information
| Parent CAS No. | 905281-76-7 |
|---|---|
| Chemical Name | 5-[1-(2-Hydroxy-ethyl)-3-pyridin-4-yl-1H-pyrazol-4-yl]-indan-1-one oxime |
| SMILES | C1N=CC=C(C2C(C3C=C4CC/C(=NO)/C4=CC=3)=CN(CCO)N=2)C=1 |
| MFCD | MFCD16875916 |
| InChi | InChI=1S/C19H18N4O2/c24-10-9-23-12-17(19(21-23)13-5-7-20-8-6-13)15-1-3-16-14(11-15)2-4-18(16)22-25/h1,3,5-8,11-12,24-25H,2,4,9-10H2/b22-18+ |
| InChiKey | DEZZLWQELQORIU-RELWKKBWSA-N |
| CID | 11717001 |
| Short Description | B-Raf inhibitor |
References
- KP Hoeflich et al. Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/MAPK pathway suppression. Cancer Res. 2009, 69(7), 3042-3051.
- H Wong et al. Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3- (pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor. J. Pharmacol. Exp. Ther. 2009, 329(1), 360-367.
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