Catalog Number: 4453
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.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GDC 0879 is reviewed on the chemical probes website.
Technical Data
  • M.Wt:
    334.37
  • Formula:
    C19H18N4O2
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    905281-76-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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 conc
    Wong et al.
    J.Pharmacol.Exp.Ther., 2009;329:360
  2. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth.
    Hatzivassiliou et al.
    Nature, 2010;464:431
  3. 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.
    Hoeflich et al.
    Cancer Res., 2009;69:3042

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