GW 5074

Cat. No. 1381 8 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent, selective c-Raf1 kinase inhibitor

化学名： 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one

纯度： ≥98% (HPLC)

说明书

引用文献 (8)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for GW 5074

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.

许可信息

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

技术数据 for GW 5074

分子量	520.94
公式	C₁₅H₈Br₂INO₂
储存	Desiccate at -20°C
纯度	≥98% (HPLC)
CAS Number	220904-83-6
PubChem ID	5924208
InChI Key	LMXYVLFTZRPNRV-KMKOMSMNSA-N
Smiles	OC(C(Br)=C1)=C(Br)C=C1/C=C(C2=CC(I)=CC=C2N3)\C3=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for GW 5074

	溶剂	最高浓度 mM
溶解性
	ethanol	1
	DMSO	100

制备储备液 for GW 5074

以下数据基于产品分子量 520.94。 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.

浓度/溶剂体积/质量	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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产品说明书 for GW 5074

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GW 5074

参考文献是支持产品生物活性的出版物。

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

Li et al (2019) Allele-selective lowering of mutant HTT protein by HTT-LC3 linker compounds. Nature 575 203 PMID: 31666698

Xue et al (2023) Discovery of a drug-like, natural product-inspired DCAF11 ligand chemotype. Nat.Commun. 14 7908 PMID: 38036533

If you know of a relevant reference for GW 5074, please let us know.

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关键词: GW 5074, GW 5074 supplier, Potent, selective, c-Raf1, kinases, inhibitors, inhibits, GW5074, mHTT, huntingtin, huntingtons, disease, Raf, Kinase, 1381, Tocris Bioscience