AG-494

• 常用名: AG-494
• 英文名: AG-494
• CAS号: 133550-35-3
• 分子量: 280.278
• 密度: 1.4±0.1 g/cm3
• 沸点: 586.9±50.0 °C at 760 mmHg
• 分子式: C₁₆H₁₂N₂O₃
• 熔点: 249 °C(dec.)
• 闪点: 308.8±30.1 °C

AG-494用途

AG-494 (Tyrphostin AG 494) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂 (IC50=0.7 μM)。AG-494 抑制EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化,IC50 为 1.1,39,45 和 6 μM。AG-494 阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。

AG-494名称

• 中文名: 酪氨酸激酶抑制剂 AG 494
• 英文名: 2-cyano-3-(3,4-dihydroxyphenyl)-N-phenylprop-2-enamide

AG-494生物活性

• 描述: AG-494 (Tyrphostin AG 494) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂 (IC50=0.7 μM)。AG-494 抑制EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化,IC50 为 1.1,39,45 和 6 μM。AG-494 阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> JAK/STAT信号通路 >> EGFR
  信号通路 >> 蛋白酪氨酸激酶 >> EGFR
  信号通路 >> 细胞周期/DNA损伤 >> CDK
• 靶点实验:

  EGFR:0.7 μM (IC50)

• 体外研究: 在DHER-14细胞中,ag494抑制Cdk2活化和EGF依赖的DNA合成[2]。AG-494显著地阻止了二氧化硅刺激细胞中NF-kB的激活,也降低了H2O2处理的细胞中NF-kB的激活[4]。AG-494(3-9μM；5-7天)以剂量依赖的方式抑制BMP9诱导的ALP活性[5]。
• 参考文献:

  [1]. Gazit A, et al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991;34(6):1896-1907.

  [2]. Osherov N, et al. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997;410(2-3):187-190.

  [3]. Osherov N, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem. 1993 May 25;268(15):11134-42.

  [4]. Liu X, Qin J, et al. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med. 2013;17(9):1160-1172.

  [5]. Jihee Lee Kang, et al. SILICA-INDUCED NUCLEAR FACTOR- k B ACTIVATION: INVOLVEMENT OF REACTIVE OXYGEN SPECIES AND PROTEIN TYROSINE KINASE ACTIVATION. Journal of Toxicology and Environmental Health, Part A.

AG-494物理化学性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 586.9±50.0 °C at 760 mmHg
• 熔点: 249 °C(dec.)
• 分子式: C₁₆H₁₂N₂O₃
• 分子量: 280.278
• 闪点: 308.8±30.1 °C
• 精确质量: 280.084778
• PSA: 93.35000
• LogP: 2.40
• InChIKey: HKHOVJYOELRGMV-XYOKQWHBSA-N
• SMILES: N#CC(=Cc1ccc(O)c(O)c1)C(=O)Nc1ccccc1
• 外观性状: 固体;Light yellow to Amber to Dark green powder to crystal
• 蒸汽压: 0.0±1.7 mmHg at 25°C
• 折射率: 1.736
• 储存条件: 0-10°C;避免光,加热

AG-494安全信息

• 危害码 (欧洲): C
• 安全声明 (欧洲): 22-24/25

AG-494靶点实验

查看更多实验

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 来源：ChEMBL 靶标：N/A External Id：CHEMBL1266185

实验名称：Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression 来源：NCGC External Id：SNCA-p-activity-luciferase

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：Tocris HTS for Inhibitors of Aerobactin Synthetase lucA 来源：23265 External Id：IucA Pilot Assay Tocris Library

实验名称：Primary Screen Inhibitors of CD40 Signaling in BL2 Cells Measured in Cell-Based Syste... 来源：Broad Institute 靶标：N/A External Id：7124-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

实验名称：Delta TM value showing the stabilisation of CAMK2G produced by compound binding 来源：ChEMBL 靶标：Calcium/calmodulin-dependent protein kinase type II subunit gamma External Id：CHEMBL3430795

实验名称：Delta TM value showing the stabilisation of CAMK4 produced by compound binding 来源：ChEMBL 靶标：Calcium/calmodulin-dependent protein kinase type IV External Id：CHEMBL3430796

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AG-494英文别名

• Tyrphostin 48
• HMS3266B19
• (2E)-2-Cyano-3-(3,4-dihydroxyphenyl)-N-phenylacrylamide
• AG-494