GW 5074

Key Product Details

Product Description

GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC₅₀ = 9 nM). GW 5074 displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fm. GW 5074 binds mutant huntingtin (mHTT) and decreases levels of mHTT in cultured hippocampal neurons and fibroblasts from patients with Huntington's disease. Brain penetrant.

Licensing Information

Sold for research purposes under agreement from Glaxo Wellcome Inc and Glaxo Group Ltd.

Product Specifications for GW 5074

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

Solubility

Preparing Stock Solutions for GW 5074

The following data is based on the product molecular weight 520.94.

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.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.92 mL	9.60 mL	19.20 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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 37 publications citing the usage of this product.

• Xue Discovery of a drug-like, natural product-inspired DCAF11 ligand chemotype. Nat.Commun. 2023 PMID: 38036533
• Li Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds. Nature 2019 PMID: 31666698
• Varga Involvement of Raf-1 in chronic delta-opioid receptor agonist-mediated adenylyl cyclase superactivation. Eur.J.Pharmacol. 2002 PMID: 12223234
• Lackey The discovery of potent cRaf1 kinase inhibitors. Bioorg.Med.Chem.Lett. 2000 PMID: 10698440
• Chen Inhibition of ATF-3 expression by B-Raf mediates the neuroprotective action of GW5074. J.Neurochem. 2008 PMID: 18194435
• Breslin VEGF increases endothelial permeability by separate signaling pathways involving ERK-1/2 and nitric oxide. Am.J.Physiol.Heart Circ.Physiol. 2003 PMID: 12388327

Product Documents for GW 5074