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GW5074

现货
Catalog No.
B1405
有效的c-Raf选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
5mg
¥ 520.00
现货
50mg
¥ 1,570.00
现货
250mg
¥ 3,140.00
现货

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Background

GW5074 is a synthetic inhibitor of c-Raf with IC50 value of 9nM [1].

GW5074 is found to be a potent inhibitor of c-Raf and has no effect on cdk1, cdk2, c-src, p38 MAP kinase, VEGFR2 and c-fms. GW5074 also shows no direct effect on JNK proteins and p38 MAP kinase. In neurons, GW5074 reduces the phosphorylation level of c-Raf at Ser259, results in an induction of c-Raf activity. It is further proved that GW5074 shows neuroprotective efficacy when its dose is below 1μM. In addition, GW5074 suppresses cell apoptosis through delaying the down-regulation of Akt phosphorylation and preventing the activation of GSK3β. In the in vivo model of Huntington’s disease, GW5074 protects neurons via resisting 3-NP-induced striatal neurodegeneration [1].

Our product is a mixture of Z and E configuration.

References:
[1] Burgess S, Echeverria V. Raf inhibitors as therapeutic agents against neurodegenerative diseases. CNS & Neurological Disorders-Drug Targets (Formerly Current Drug Targets-CNS & Neurological Disorders), 2010, 9(1): 120-127.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt520.94
Cas No.220904-83-6
FormulaC15H8Br2INO2
Solubility>26.1mg/mL in DMSO
Chemical Name3-(3,5-dibromo-4-hydroxybenzylidene)-5-iodoindolin-2-one
SDFDownload SDF
Canonical SMILESIC1=CC=C(NC(C2=CC3=CC(Br)=C(O)C(Br)=C3)=O)C2=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

小脑颗粒神经元

溶解方法

该化合物在DMSO中的溶解度大于26.1 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1 μM,40 min

应用

用GW5074处理神经元导致c-Raf激活,刺激Raf-MEK-ERK通路。GW5074处理神经元增加B-Raf的活性。GW5074抑制颗粒细胞和其他神经元类型中神经毒素引起的细胞死亡。

动物实验 [1,2]:

动物模型

具有亨廷顿氏病(HD)的C57BL/6雄性小鼠,每天反复暴露在四支烟造成的烟雾环境中的小鼠,暴露4周

给药剂量

腹腔注射,2 mg/kg,每天给药,三周

应用

GW5074(5 mg/kg)完全阻止了C57BL/6雄性小鼠中3-NP诱导的大面积双侧纹状体损伤。GW5074(0.5 mg/kg或2 mg/kg)抑制小鼠的侧流烟雾引起的气道高反应性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Chin P C, Liu L, Morrison B E, et al. The c‐Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK‐ERK and Akt‐independent mechanism[J]. Journal of neurochemistry, 2004, 90(3): 595-608.

[2]. Lei Y, Cao Y X, Xu C B, et al. The Raf-1 inhibitor GW5074 and dexamethasone suppress sidestream smoke-induced airway hyperresponsiveness in mice[J]. Respiratory research, 2008, 9(1): 71.

生物活性

Description GW5074是有效的c-Raf选择性抑制剂,其IC50值为9 nM.
靶点 C-Raf          
IC50 9 nM          

质量控制

化学结构

GW5074