GW 5074 | Raf-1 Inhibitor | AmBeed-信号通路专用抑制剂

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GW 5074 {[allProObj[0].p_purity_real_show]}

货号：A471753

GW5074 is an inhibitor of c-Raf1 kinase with IC50 of 9 nM.

GW 5074 化学结构
CAS号：220904-83-6

GW 5074 3D分子结构
CAS号：220904-83-6

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GW 5074 纯度/质量文件产品仅供科研

货号：A471753 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

Raf 亚型比较

产品名称	A-raf ↓ ↑	B-Raf ↓ ↑	C-Raf/Raf-1 ↓ ↑	Raf ↓ ↑	其他靶点	纯度
Encorafenib		✔				99%+
GDC-0879		++++ B-Raf, IC50: 0.13 nM				99%+
SB-590885		++++ B-Raf, Ki: 0.16 nM				99%+
RAF265						99%+
Dabrafenib		++++ B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM	+++ C-Raf, IC50: 6.3 nM			98%
Lifirafenib	++++ WT A-RAF, IC50: 1 nM	++ BRAF(V600E), IC50: 23 nM BRAF WT, IC50: 32 nM	+++ C-RAF (Y340/341D), IC50: 7 nM		EGFR	98%
ZM 336372			+ C-Raf, IC50: 70 nM			99%+
NVP-BHG 712			+ C-Raf, IC50: 0.395 μM			99%+
CCT196969		+ BRAF, IC50: 0.1 μM	++ CRAF, IC50: 0.01 μM		Src	98%
Vemurafenib		++ B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM	+ C-Raf, IC50: 48 nM			98+%
PLX4720		++ B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM	+++ C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM		BRK	99+%
GW 5074			+++ C-Raf, IC50: 9 nM			99%+
Avutometinib		+++ BRAF V600E, IC50: 8.2 nM BRAF, IC50: 19 nM	+ CRAF, IC50: 56 nM			98%
LY3009120		++++ BRAF(V600E), IC50: 5.8 nM BRAF WT, IC50: 15 nM	++++ C-Raf, IC50: 4.3 nM			99%+
Agerafenib		++ B-Raf (V600E), Kd: 14 nM B-Raf, Kd: 36 nM	+ C-Raf, Kd: 39 nM		RET	99%+
TAK-632		+++ B-Raf, IC50: 8.3 nM	++++ C-Raf, IC50: 1.4 nM			99%+
AZ 628		+ B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM	++ C-Raf-1, IC50: 29 nM			99%
PLX7904				✔		98+%
Sorafenib		++ B-Raf (V599E), IC50: 38 nM B-Raf, IC50: 22 nM	++++ Raf-1, IC50: 6 nM	++++ Raf-1, IC50: 6 nM		99%
Tovorafenib				✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GW 5074 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].

GW 5074 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.

GW 5074 实验方案

计算器

存储液制备

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

GW 5074 技术信息

CAS号	220904-83-6
分子式	C₁₅H₈Br₂INO₂
分子量	520.942

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

GW 5074 {[allProObj[0].p_purity_real_show]}

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GW 5074 {[allProObj[0].p_purity_real_show]}

GW 5074 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GW 5074 质控信息

GW 5074 生物活性

GW 5074 参考文献

GW 5074 实验方案

GW 5074 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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GW 5074 纯度/质量文件产品仅供科研