847499-27-8

• 常用中文名：Delanzomib
• 常用英文名：CEP-18770 (Delanzomib)
• CAS号：847499-27-8
• 分子式：C₂₁H₂₈BN₃O₅
• 分子量：413.275
• 相关类别： 生物化工 抑制剂 蛋白酶体(Proteases) Proteasome 抑制剂
• 发布时间：2018-12-12 17:50:48
• 更新时间：2024-01-07 14:38:48
• Delanzomib(CEP-18770)是口服活性的蛋白酶体糜蛋白酶样活性抑制剂,能下调核内NF-kappaB活性。

名称

• 中文名: [(1R)-1-[[(2S,3R)-3-羟基-1-氧代-2-[[(6-苯基-2-吡啶基)羰基]氨基]丁基]氨基]-3-甲基丁基]硼酸
• 英文名: ((R)-1-((2S,3R)-3-Hydroxy-2-(6-phenylpicolinamido)butanamido)-3-methylbutyl)boronic acid
• 英文别名: Delanzomib; B-[(1R)-1-({N-[(6-phenylpyridin-2-yl)carbonyl]-L-threonyl}amino)-3-methylbutyl]boronic acid; Boronic acid, B-[(1R)-1-[[(2S,3R)-3-hydroxy-1-oxo-2-[[(6-phenyl-2-pyridinyl)carbonyl]amino]butyl]amino]-3-methylbutyl]-; [(1R)-3-Methyl-1-({N-[(6-phenyl-2-pyridinyl)carbonyl]-L-threonyl} amino)butyl]boronic acid; B-[(1R)-1-[[(2S,3R)-3-hydroxy-1-oxo-2-[[(6-phenyl-2- pyridinyl)carbonyl]amino]butyl]amino]-3-methylbutyl]boronic acid; [(1R)-3-Methyl-1-({N-[(6-phenyl-2-pyridinyl)carbonyl]-L-threonyl}amino)butyl]boronic acid; CEP-18770

物化性质

• 密度: 1.207
• 分子式: C₂₁H₂₈BN₃O₅
• 分子量: 413.275
• 精确质量: 413.212189
• PSA: 138.76000
• LogP: 2.89
• 外观性状: 粉末
• 折射率: 1.563
• 储存条件: -20℃

生物活性

• 描述: Delanzomib(CEP-18770)是口服活性的蛋白酶体糜蛋白酶样活性抑制剂,能下调核内NF-kappaB活性。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体
  研究领域 >> 癌症
• 参考文献:

  [1]. Piva R, et al. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib. Blood. 2008 Mar 1;111(5):2765-75.

  [2]. Sanchez E, et al. The proteasome inhibitor CEP-18770 enhances the anti-myeloma activity of bortezomib and melphalan. Br J Haematol. 2010 Feb;148(4):569-81.

  [3]. Seavey MM, et al. Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE. Int Immunopharmacol. 2012 Jan;12(1):257-70.

  [4]. Gallerani E, et al. A first in human phase I study of the proteasome inhibitor CEP-18770 in patients with advanced solid tumours and multiple myeloma. Eur J Cancer. 2013 Jan;49(2):290-6.