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GDC 0879Cat. No. 4453 |
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Chemical Name: (E)-2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one oxime |
Biological Activity
Potent and selective B-Raf inhibitor (IC50 = 0.13 nM against purified B-Raf V600E). Activity reduces phospho-ERK (pERK) levels (IC50 = 63 nM in the Malme-3M cell line). Inhibits the Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines. Does not activate apoptotic pathways in A375 or Colo205 cell lines. Orally bioavailable.Certificate of Analysis / Safety Data Sheet
References
Hoeflich et al (2009) 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. 69 3042. PMID: 19276360.
Wong et al (2009) 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. 329 360. PMID: 19147858.
Hatzivassiliou et al (2010) RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 464 431. PMID: 20130576.
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Keywords: GDC 0879, supplier, GDC0879, b-raf, braf, inhibitors, potent, selective
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