GDC 0879
Tocris Bioscience, part of Bio-Techne | Catalog # 4453
Potent B-Raf inhibitor
Product Description
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.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.Product Specifications
Molecular Weight
334.37
Formula
C19H18N4O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
2,3-Dihydro-5-[1-(2-hydroxyethyl)-3-(4-pyridinyl)-1H-pyrazol-4-yl]-1H-inden-1-one oxime
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.34 | 10 |
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 all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 29.91 mL | 149.53 mL | 299.07 mL |
| 0.5 mM | 5.98 mL | 29.91 mL | 59.81 mL |
| 1 mM | 2.99 mL | 14.95 mL | 29.91 mL |
| 5 mM | 0.60 mL | 2.99 mL | 5.98 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
- Hoeflich 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. 2009 PMID: 19276360
- 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
Product Specific Notices for GDC 0879
For research use only
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