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.
| Cas No. | 905281-76-7 |
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| 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 66 mg/mL warmed (197.38 mM) Ethanol 5 mg/mL (14.95 mM) Water Insoluble |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet | |
| Brochures |
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.
