468740-43-4

• 常用中文名：胰岛素样生长因子-1 受体拮抗剂
• 常用英文名：BMS-536924
• CAS号：468740-43-4
• 分子式：C₂₅H₂₆ClN₅O₃
• 分子量：479.959
• 相关类别： 生物化工 抑制剂 蛋白酪氨酸激酶
• 发布时间：2018-12-06 22:47:51
• 更新时间：2024-01-08 14:39:14
• BMS-536924是ATP竞争性IGF-1R/IR抑制剂, IC50分别为100 nM/73 nM。

名称

• 中文名: 胰岛素样生长因子-1 受体拮抗剂
• 英文名: (S)-4-[2-(3-Chloro-phenyl)-2-hydroxy-ethylamino]-3-(4-methyl-6-morpholin-4-yl-1H-benzoimidazol-2-yl)-1H-pyridin-2-one
• 英文别名: CDK inhibitor; 4-{[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}-3-[4-methyl-6-(morpholin-4-yl)-1H-benzimidazol-2-yl]pyridin-2(1H)-one; 4-{[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino}-3-[4-methyl-6-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone; CHEMBL401930; 4-[[(2S)-2-(3-CHLOROPHENYL)-2-HYDROXYETHYL]AMINO]-3-[7-METHYL-5-(4-MORPHOLINYL)-1H-BENZIMIDAZOL-2-YL]-2(1H)-PYRIDINONE; 2(1H)-Pyridinone, 4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-3-[4-methyl-6-(4-morpholinyl)-1H-benzimidazol-2-yl]-; INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR INHIBITOR; BMS-536924

物化性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₂₅H₂₆ClN₅O₃
• 分子量: 479.959
• 精确质量: 479.172424
• PSA: 106.27000
• LogP: 2.61
• 外观性状: 粉末
• 折射率: 1.717
• 储存条件: -20℃

生物活性

• 描述: BMS-536924是ATP竞争性IGF-1R/IR抑制剂, IC50分别为100 nM/73 nM。
• 相关类别:
  信号通路 >> 蛋白酪氨酸激酶 >> IGF-1R
  信号通路 >> 蛋白酪氨酸激酶 >> 胰岛素受体
  研究领域 >> 癌症
• 参考文献:

  [1]. Wittman M, et al. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem. 2005 Sep 8;48(18):5639-43.

  [2]. Litzenburger BC, et al. BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells. Clin Cancer Res. 2009 Jan 1;15(1):226-37.

  [3]. Ohashi H, et al. Insulin-like growth factor receptor expression is associated with aggressive phenotypes and has therapeutic activity in biliary tract cancers. Cancer Sci. 2012 Feb;103(2):252-61.

合成路线

468741-20-0 ~% 468740-43-4

文献：Wittman, Mark; Carboni, Joan; Attar, Ricardo; Balasubramanian, Balu; Balimane, Praveen; Brassil, Patrick; Beaulieu, Francis; Chang, Chiehying; Clarke, Wendy; Dell, Janet; Eummer, Jeffrey; Frennesson, David; Gottardis, Marco; Greer, Ann; Hansel, Steven; Hurlburt, Warren; Jacobson, Bruce; Krishnananthan, Subramaniam; Lee, Francis Y.; Li, Aixin; Lin, Tai-An; Liu, Peiying; Ouellet, Carl; Sang, Xiaopeng; Saulnier, Mark G.; Stoffan, Karen; Sun, Yax; Velaparthi, Upender; Wong, Henry; Yang, Zheng; Zimmermann, Kurt; Zoeckler, Mary; Vyas, Dolatrai Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5639 - 5643

77811-44-0 ~% 468740-43-4

文献：Wittman, Mark; Carboni, Joan; Attar, Ricardo; Balasubramanian, Balu; Balimane, Praveen; Brassil, Patrick; Beaulieu, Francis; Chang, Chiehying; Clarke, Wendy; Dell, Janet; Eummer, Jeffrey; Frennesson, David; Gottardis, Marco; Greer, Ann; Hansel, Steven; Hurlburt, Warren; Jacobson, Bruce; Krishnananthan, Subramaniam; Lee, Francis Y.; Li, Aixin; Lin, Tai-An; Liu, Peiying; Ouellet, Carl; Sang, Xiaopeng; Saulnier, Mark G.; Stoffan, Karen; Sun, Yax; Velaparthi, Upender; Wong, Henry; Yang, Zheng; Zimmermann, Kurt; Zoeckler, Mary; Vyas, Dolatrai Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5639 - 5643

21886-56-6 ~% 468740-43-4

文献：Wittman, Mark; Carboni, Joan; Attar, Ricardo; Balasubramanian, Balu; Balimane, Praveen; Brassil, Patrick; Beaulieu, Francis; Chang, Chiehying; Clarke, Wendy; Dell, Janet; Eummer, Jeffrey; Frennesson, David; Gottardis, Marco; Greer, Ann; Hansel, Steven; Hurlburt, Warren; Jacobson, Bruce; Krishnananthan, Subramaniam; Lee, Francis Y.; Li, Aixin; Lin, Tai-An; Liu, Peiying; Ouellet, Carl; Sang, Xiaopeng; Saulnier, Mark G.; Stoffan, Karen; Sun, Yax; Velaparthi, Upender; Wong, Henry; Yang, Zheng; Zimmermann, Kurt; Zoeckler, Mary; Vyas, Dolatrai Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5639 - 5643

174699-78-6 ~% 468740-43-4

文献：Wittman, Mark; Carboni, Joan; Attar, Ricardo; Balasubramanian, Balu; Balimane, Praveen; Brassil, Patrick; Beaulieu, Francis; Chang, Chiehying; Clarke, Wendy; Dell, Janet; Eummer, Jeffrey; Frennesson, David; Gottardis, Marco; Greer, Ann; Hansel, Steven; Hurlburt, Warren; Jacobson, Bruce; Krishnananthan, Subramaniam; Lee, Francis Y.; Li, Aixin; Lin, Tai-An; Liu, Peiying; Ouellet, Carl; Sang, Xiaopeng; Saulnier, Mark G.; Stoffan, Karen; Sun, Yax; Velaparthi, Upender; Wong, Henry; Yang, Zheng; Zimmermann, Kurt; Zoeckler, Mary; Vyas, Dolatrai Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5639 - 5643

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