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GW 5074

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Chemical Structure| 220904-83-6 同义名 : -
CAS号 : 220904-83-6
货号 : A471753
分子式 : C15H8Br2INO2
纯度 : 99%+
分子量 : 520.942
MDL号 : MFCD09971042
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(201.56 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 1.6 mg/mL clear

PO 0.5% CMC-Na 51 mg/mL suspension

生物活性
靶点

  • C-Raf/Raf-1

    C-Raf, IC50:9 nM
描述 The mammalian Raf kinase family consists of A-Raf and B-Raf and c-Raf (or Raf 1). The c-Raf has been proven an upstream activator of mitogen-activated protein kinase (MAPK), which is an important group of mediators transducing signals from cell surface to nucleus under stimuli including cytokines, growth factors, exogenous pressure and mitogens. The RAF was also proven to be an oncogenic gene that was closely associated with tumorigenesis[3]. GW5074 is a potent inhibitor of c-Raf with an IC50 value of 9 nM. Treatment with GW5074 for 24 hours prevents LK-induced apoptosis in medium containing LK. Maximal protection against LK-induced apoptosis is observed at 1 μM. The activity of c-Raf immunoprecipitated from cultures treated with GW5074 in LK medium displayed a marked induction. Dispite its inhibition of c-Raf, treatment of neuronal cultures with GW5074 lea to an increase in the phosphorylation of ERK 1/2 suggesting that GW5074 treatment caused the activation of either A-Raf or B-Raf. Mice administered 3-NP display extensive bilateral striatal lesions. This degeneration is completely prevented by GW5074 when administered at a concentration of 5 mg/kg body weight[4].
作用机制 c-Raf is inhibited by phosphorylation at Ser259 with GW5074[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.60mL

1.92mL

0.96mL

19.20mL

3.84mL

1.92mL
参考文献

[1]Lei Y, Cao YX, et al. The Raf-1 inhibitor GW5074 and dexamethasone suppress sidestream smoke-induced airway hyperresponsiveness in mice. Respir Res. 2008 Nov 3;9:71.

[2]Yue X, Varga EV, et al. Chronic morphine-mediated adenylyl cyclase superactivation is attenuated by the Raf-1 inhibitor, GW5074. Eur J Pharmacol. 2006 Jul 1;540(1-3):57-9.

[3]Wei X, Zhao T, Ai K, Zhang Y, Li H, Yang J. c-Raf participates in adaptive immune response of Nile tilapia via regulating lymphocyte activation. Fish Shellfish Immunol. 2019;86:507-515.

[4]Chin PC, Liu L, Morrison BE, 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 Neurochem. 2004;90(3):595-608.