GDC-0879
GDC-0879 is an orally bioavailable kinase inhibitor that exhibits anticancer chemotherapeutic activity in vitro and in vivo. GDC-0879 inhibits mutant (V600E) B-Raf, a mutation common to many types of cancer. This inhibition of mutant B-Raf decreases MEK1 phosphorylation, downregulating expression of genes associated with cell proliferation and resulting in sustained inhibition of tumor cell proliferation.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18926325
| Cas No. |
905281-76-7 |
|---|---|
| Purity |
≥96% |
| Formula |
C19H18N4O2 |
| Formula Wt. |
334.37 |
| Chemical Name |
(E)-5-(1-(2-hydroxyethyl)-3-(pyridin-4-yl)-1H-pyrazol-4-yl)-2,3-dihydroinden-1-one oxime |
| IUPAC Name |
2-[4-[(1E)-1-hydroxyimino-2,3-dihydroinden-5-yl]-3-pyridin-4-ylpyrazol-1-yl]ethanol |
| Solubility |
DMSO 67 mg/mL |
Hoeflich KP, Herter S, Tien J, et al. Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression. Cancer Res. 2009 Apr 1;69(7):3042-51. PMID: 19276360.
Wong H, Belvin M, Herter S, 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: understanding relationships between systemic concentrations, phosphorylated mitogen-activated protein kinase kinase 1 inhibition, and efficacy. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7. PMID: 19147858.
