GDC 0879

Name: GDC 0879
Brand: Tocris Bioscience
SKU: 4453

Tocris Bioscience a Bio-Techne Brand

Catalog # 4453

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Key Product Details

Description:	Potent B-Raf inhibitor
Chemical Name:	2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one oxime
Purity:	≥98% (HPLC)
Molecular Weight:	334.37

View Full Technical Details for GDC 0879

Biological Activity for GDC 0879

GDC 0879 is a 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.

Compound Libraries for GDC 0879

GDC 0879 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

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 for GDC 0879

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 for GDC 0879

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

Preparing Stock Solutions for GDC 0879

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	0.60 mL	2.99 mL	5.98 mL
10 mM	0.30 mL	1.50 mL	2.99 mL
50 mM	0.06 mL	0.30 mL	0.60 mL

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References for GDC 0879

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

Hatzivassiliou RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 2010 PMID: 20130576
Wong 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. 2009 PMID: 19147858
Hoeflich Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAF^V600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression. Cancer Res. 2009 PMID: 19276360

Citations for GDC 0879

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