Biological Activity
Potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM). Displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm.
Licensing Information
Sold for research purposes under agreement from Glaxo Wellcome Inc and Glaxo Group Ltd.
Technical Data
| M. Wt | 520.94 |
| Formula | C15H8Br2INO2 |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 220904-83-6 |
| PubChem ID | 5924208 |
| InChI Key | LMXYVLFTZRPNRV-KMKOMSMNSA-N |
| Smiles | OC1=C(Br)C=C(C=C2/C(=O)NC3=CC=C(I)C=C23)C=C1Br |
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.
Solubility Data
| Solubility | Soluble to 1 mM in ethanol and to 100 mM in DMSO |
Preparing Stock Solutions
The following data is based on the product molecular weight 520.94. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 1.92 mL | 9.6 mL | 19.2 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.84 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.92 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Breslin et al (2003) VEGF increases endothelial permeability by separate signaling pathways involving ERK-1/2 and nitric oxide. Am.J.Physiol.Heart Circ.Physiol. 284 H92 PMID: 12388327
Chen et al (2008) Inhibition of ATF-3 expression by B-Raf mediates the neuroprotective action of GW5074. J.Neurochem. 105 1300 PMID: 18194435
Lackey et al (2000) The discovery of potent cRaf1 kinase inhibitors. Bioorg.Med.Chem.Lett. 10 223 PMID: 10698440
Varga et al (2002) Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation. Eur.J.Pharmacol. 451 101 PMID: 12223234
Keywords: GW 5074, supplier, Potent, selective, c-Raf1, kinases, inhibitors, inhibits, GW5074, Raf, Kinase, Raf, Kinase, Tocris Bioscience
