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Submit ReviewGDC 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.
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.
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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 33.44 | 100 |
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 |
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
If you know of a relevant reference for GDC 0879, please let us know.
Keywords: GDC 0879, GDC 0879 supplier, GDC0879, b-raf, braf, inhibitors, inhibits, potent, selective, Raf, Kinase, 4453, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for GDC 0879 include:
Konstantinos et al (2021) Cdk5 and GSK3β inhibit fast endophilin-mediated endocytosis. Nat Commun 12 2424 PMID: 33893293
Do you know of a great paper that uses GDC 0879 from Tocris? Please let us know.
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