GDC 0879

Cat. No. 4453

GDC 0879 C19H18N4O2 [905281-76-7]

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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.

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View 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.

If you know of a relevant citation for this product please let us know.

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Keywords: GDC 0879, supplier, GDC0879, b-raf, braf, inhibitors, potent, selective, Tocris Bioscience, Raf Kinase Inhibitors

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