GDC 0879

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Cat.No. 4453 - GDC 0879 | C19H18N4O2 | CAS No. 905281-76-7
Description: Potent B-Raf inhibitor
Chemical Name: (E)-2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one oxime
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

GDC 0879 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 334.37
Formula C19H18N4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 905281-76-7
PubChem ID 11717001
InChI Key DEZZLWQELQORIU-RELWKKBWSA-N
Smiles OCCN1N=C(C3=CC=NC=C3)C(C2=CC=C(/C(CC4)=N/O)C4=C2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.44 100

Preparing Stock Solutions

The following data is based on the product molecular weight 334.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.99 mL 14.95 mL 29.91 mL
5 mM 0.6 mL 2.99 mL 5.98 mL
10 mM 0.3 mL 1.5 mL 2.99 mL
50 mM 0.06 mL 0.3 mL 0.6 mL

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References

References are publications that support the biological activity of the product.

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 conc 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

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


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