N-(2,6-二氟苯基)-5-[3-[2-[[5-乙基-2-甲氧基-4-[4-[4-(甲基磺酰基)-1-哌嗪基]-1-哌啶基]苯基]氨基]-4-嘧啶基]咪唑并[1,2-A]吡啶-2-基]-2-甲氧基苯甲酰胺

• 常用名: N-(2,6-二氟苯基)-5-[3-[2-[[5-乙基-2-甲氧基-4-[4-[4-(甲基磺酰基)-1-哌嗪基]-1-哌啶基]苯基]氨基]-4-嘧啶基]咪唑并[1,2-A]吡啶-2-基]-2-甲氧基苯甲酰胺
• 英文名: GSK1904529A
• CAS号: 1089283-49-7
• 分子量: 851.963
• 密度: 1.4±0.1 g/cm3
• 沸点: N/A
• 分子式: C₄₄H₄₇F₂N₉O₅S
• 熔点: N/A
• 闪点: N/A

用途

GSK1904529A是IGF-1R和IR的选择性抑制剂,IC50分别为27 nM和25 nM,对Akt1/2,Aurora A/B,B-Raf,CDK2,EGFR的抑制性相对较弱。

名称

• 中文名: N-(2,6-二氟苯基)-5-[3-[2-[[5-乙基-2-甲氧基-4-[4-[4-(甲基磺酰基)-1-哌嗪基]-1-哌啶基]苯基]氨基]-4-嘧啶基]咪唑并[1,2-A]吡啶-2-基]-2-甲氧基苯甲酰胺
• 英文名: N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide

生物活性

• 描述: GSK1904529A是IGF-1R和IR的选择性抑制剂,IC50分别为27 nM和25 nM,对Akt1/2,Aurora A/B,B-Raf,CDK2,EGFR的抑制性相对较弱。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> IGF-1R
  研究领域 >> 癌症
• 参考文献:

  [1]. Sabbatini P, et al. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res, 2009, 15(9), 3058-3067.

物理化学性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₄₄H₄₇F₂N₉O₅S
• 分子量: 851.963
• 精确质量: 851.338867
• PSA: 158.40000
• LogP: 4.69
• InChIKey: MOSKATHMXWSZTQ-UHFFFAOYSA-N
• SMILES: CCc1cc(Nc2nccc(-c3c(-c4ccc(OC)c(C(=O)Nc5c(F)cccc5F)c4)nc4ccccn34)n2)c(OC)cc1N1CCC(N2CCN(S(C)(=O)=O)CC2)CC1
• 外观性状: 粉末
• 折射率: 1.672
• 储存条件: -20℃

靶点实验

查看更多实验

实验名称：Inhibition of N-terminal His6-tagged recombinant full-length human TBK1 expressed in ... 来源：ChEMBL 靶标：Serine/threonine-protein kinase TBK1 External Id：CHEMBL5679589

实验名称：Inhibition of N-terminal 6His-tagged recombinant human TAO3 (1 to 411 residues) expre... 来源：ChEMBL 靶标：Serine/threonine-protein kinase TAO3 External Id：CHEMBL5679588

实验名称：Inhibition of N-terminal 6His-tagged recombinant human TLK2 (388 to end residues) exp... 来源：ChEMBL 靶标：Serine/threonine-protein kinase tousled-like 2 External Id：CHEMBL5679591

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：Inhibition of N-terminal His6-tagged recombinant human Tie2 (771 to end residues) exp... 来源：ChEMBL 靶标：Angiopoietin-1 receptor External Id：CHEMBL5679590

实验名称：Inhibition of N-terminal His6 tagged recombinant human TrkB (455 to end residues) exp... 来源：ChEMBL 靶标：BDNF/NT-3 growth factors receptor External Id：CHEMBL5679593

实验名称：Inhibition of N-terminal His6-tagged recombinant human TrkA (440 to end residues) exp... 来源：ChEMBL 靶标：High affinity nerve growth factor receptor External Id：CHEMBL5679592

实验名称：Inhibition of N-terminal His6-tagged recombinant full length human TSSK2 expressed in... 来源：ChEMBL 靶标：Testis-specific serine/threonine-protein kinase 2 External Id：CHEMBL5679595

实验名称：Inhibition of 6His-tagged recombinant human full length TSSK1 expressed in baculoviru... 来源：ChEMBL 靶标：Testis-specific serine/threonine-protein kinase 1 External Id：CHEMBL5679594

实验名称：Ratio of IC50 for inhibition of IGF1R in human ANBL6 cells assessed as reduction of c... 来源：ChEMBL 靶标：Insulin-like growth factor 1 receptor External Id：CHEMBL5720029

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英文别名

• gsk1904529a
• N-(2,6-Difluorophenyl)-5-(3-{2-[(5-ethyl-2-methoxy-4-{4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl}phenyl)amino]-4-pyrimidinyl}imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide