EW-7197

• 常用名: EW-7197
• 英文名: Vactosertib (TEW-7197)
• CAS号: 1352608-82-2
• 分子量: 399.424
• 密度: 1.4±0.1 g/cm3
• 沸点: N/A
• 分子式: C₂₂H₁₈FN₇
• 熔点: N/A
• 闪点: N/A

EW-7197用途

Vactosertib (EW-7197) 是 ALK5 的 ATP 竞争性抑制剂,IC50 为 12.9 nM。抑制 ALK2 和 ALK4 在纳摩尔级别。

EW-7197名称

• 中文名: N-[[4-([1,2,4]三唑并[1,5-a]吡啶-6-基)-5-(6-甲基吡啶-2-基)-1H-咪唑-2-基]甲基]-2-氟苯胺
• 英文名: 1H-​Imidazole-​2-​methanamine, N-​(2-​fluorophenyl)​-​5-​(6-​methyl-​2-​pyridinyl)​-​4-​[1,​2,​4]​triazolo[1,​5-​a]​pyridin-​6-​yl

EW-7197生物活性

• 描述: Vactosertib (EW-7197) 是 ALK5 的 ATP 竞争性抑制剂,IC50 为 12.9 nM。抑制 ALK2 和 ALK4 在纳摩尔级别。
• 相关类别:
  信号通路 >> TGF-beta/Smad 信号通路 >> TGF-β受体
  研究领域 >> 癌症
• 靶点实验:

  IC50: 12.9 nM (TRPV4)[1]

• 参考文献:

  [1]. Jin CH et al. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem, 2014 May 22, 57(10):4213-38.

  [2]. Son JY et al. EW-7197, a novel ALK-5 kinase inhibitor, potently inhibits breast to lung metastasis, 2014 Jul, 13(7):1704-16.

  [3]. Yoon JH et al. Activin receptor-like kinase5 inhibition suppresses mouse melanoma by ubiquitin degradation of Smad4,thereby derepressing eomesodermin in cytotoxic T lymphocytes. EMBO Mol Med, 2013 Nov, 5(11):1720-39.

EW-7197物理化学性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₂₂H₁₈FN₇
• 分子量: 399.424
• 精确质量: 399.160767
• PSA: 83.79000
• LogP: 3.19
• InChIKey: FJCDSQATIJKQKA-UHFFFAOYSA-N
• SMILES: Cc1cccc(-c2[nH]c(CNc3ccccc3F)nc2-c2ccc3ncnn3c2)n1
• 外观性状: 粉末
• 折射率: 1.725
• 储存条件: -20℃

EW-7197靶点实验

查看更多实验

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Receptor-interacting serine/threonine-protein kinase 2 External Id：CHEMBL5478927

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Platelet-derived growth factor receptor alpha External Id：CHEMBL5478926

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Platelet-derived growth factor receptor alpha External Id：CHEMBL5478925

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Misshapen-like kinase 1 External Id：CHEMBL5478924

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Mitogen-activated protein kinase kinase kinase kinase 4 External Id：CHEMBL5478923

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Vascular endothelial growth factor receptor 2 External Id：CHEMBL5478921

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Vascular endothelial growth factor receptor 3 External Id：CHEMBL5478920

实验名称：Selectivity interaction (Kinase panel (radiometric 33ProQinase Activity Assays, singl... 来源：ChEMBL 靶标：Vascular endothelial growth factor receptor 1 External Id：CHEMBL5478919

实验名称：Selectivity index, ratio of IC50 for human recombinant untagged p38aplha to IC50 for ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4434541

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EW-7197英文别名

• 2-Fluoro-N-{[4-(6-methyl-2-pyridinyl)-5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-1H-imidazol-2-yl]methyl}aniline
• EW-7197
• N-[[4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl]methyl]-2-fluoroaniline
• TEW-7197