253128-41-5

• 常用中文名：艾日布林
• 常用英文名：Eribulin
• CAS号：253128-41-5
• 分子式：C₄₀H₅₉NO₁₁
• 分子量：729.897
• 相关类别： 信号通路 细胞周期/DNA损伤 微管/微管蛋白
• 发布时间：2018-08-04 18:21:47
• 更新时间：2024-01-03 10:29:20
• Eribulin (E7389; ER-086526)是合成的软海绵素B类似物,能结合微管蛋白和微管,已进入抗乳腺癌三期临床实验。

名称

• 中文名: 艾瑞布林
• 英文名: eribulin
• 中文别名: 甲磺酸艾日布林; 艾日布林
• 英文别名: Cyclopentanecarboxylicacid,3-[[(1,1-dimethylethoxy)carbonyl]amino]-4-hydroxy-,methyl ester,(1S,3S,4R); Eribulin; (1S,3S,4R)-3-tert-butoxycarbonylamino-4-hydroxycyclopentanecarboxylic acid methyl ester; 2-(3-Amino-2-hydroxypropyl)hexacosahydro-3-methoxy- 26-methyl-20,27-bis(methylene)11,15-18,21-24,28-triepoxy- 7,9-ethano-12,15-methano-9H,15H-furo(3,2-i)furo(2',3'-5,6) pyrano(4,3-b)(1,4)dioxacyclopentacosin-5-(4H)-one; NSC-707389; Methyl(1S,3S,4R)NBOC3amino4hydroxycyclopentanecarboxylate; Halaven; (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33S,35R,36S)-20-[(2S)-3-Amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-bis(methylene)-2,19,30,34,37,39,40,41-octaoxanonacyclo[24.9.2.1. 1.1.1.0.0.0]hentetracontan-24-one; ER-086526; (1S,3S,6S,9S,12S,14R,16R,18S,20R,21R,22S,26R,29S,31R,32S,33R,35R,36S)-20-[(2S)-3-Amino-2-hydroxypropyl]-21-methoxy-14-methyl-8,15-bis(methylene)-2,19,30,34,37,39,40,41-octaoxanonacyclo [24.9.2.13,32.13,33.16,9.112,16.018,22.029,36.031,35]hentetracontan-24-one

物化性质

• 密度: 1.29±0.1 g/cm3
• 分子式: C₄₀H₅₉NO₁₁
• 分子量: 729.897
• 精确质量: 729.408813
• PSA: 146.39000
• LogP: 3.88
• 折射率: 1.584
• 储存条件: 2-8℃
• 水溶解性: Practically insoluble (0.015 g/L) (25 ºC)

生物活性

• 描述: Eribulin (E7389; ER-086526)是合成的软海绵素B类似物,能结合微管蛋白和微管,已进入抗乳腺癌三期临床实验。
• 相关类别:
  信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白
  信号通路 >> 细胞骨架 >> 微管/微管蛋白
  研究领域 >> 癌症
• 参考文献:

  [1]. Okouneva, T., et al., Inhibition of centromere dynamics by eribulin (E7389) during mitotic metaphase. Mol Cancer Ther, 2008. 7(7): p. 2003-11.

  [2]. Smith, J.A., et al., Eribulin binds at microtubule ends to a single site on tubulin to suppress dynamic instability. Biochemistry, 2010. 49(6): p. 1331-7.

  [3]. Towle, M.J., et al., Eribulin induces irreversible mitotic blockade: implications of cell-based pharmacodynamics for in vivo efficacy under intermittent dosing conditions. Cancer Res, 2011. 71(2): p. 496-505.