1392136-43-4

• 常用中文名：Verdinexor
• 常用英文名：Verdinexor
• CAS号：1392136-43-4
• 分子式：C₁₈H₁₂F₆N₆O
• 分子量：442.318
• 相关类别： 生物化工 抑制剂 跨膜转运体(Transmembrane Transporters) CRM1 抑制剂
• 发布时间：2016-07-12 13:52:13
• 更新时间：2024-01-06 12:11:41
• Verdinexor(KPT-335)是新型口服活性出核抑制剂(SINE),能有效抑制犬肿瘤细胞系出核蛋白Exportin 1(XPO1/CRM1),也能降低流感病毒的复制水平。

名称

• 中文名: Verdinexor
• 英文名: (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyridin-2-ylprop-2-enehydrazide
• 英文别名: Verdinexor [INN]; verdinexor; 2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyridinyl)hydrazide, (2Z)-; (2Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)prop-2-enehydrazide; KPT-335; (2Z)-3-{3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}-N'-(2-pyridinyl)acrylohydrazide; 2-Propenoic acid,3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-,2-(2-pyridinyl)hydrazide,(2Z)

物化性质

• 密度: 1.5±0.1 g/cm3
• 分子式: C₁₈H₁₂F₆N₆O
• 分子量: 442.318
• 精确质量: 442.097687
• PSA: 88.22000
• LogP: 4.10
• 外观性状: 粉末
• 折射率: 1.577
• 储存条件: -20℃

生物活性

• 描述: Verdinexor(KPT-335)是新型口服活性出核抑制剂(SINE),能有效抑制犬肿瘤细胞系出核蛋白Exportin 1(XPO1/CRM1),也能降低流感病毒的复制水平。
• 相关类别:
  信号通路 >> 跨膜转运 >> CRM1
  研究领域 >> 癌症
• 参考文献:

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  [2]. Pohl O, et al. Carcinogenicity and chronic rodent toxicity of the selective progesterone receptor modulator ulipristal acetate. Curr Drug Saf. 2013 Apr;8(2):77-97.

  [3]. Pohl O, et al. A 39-week oral toxicity study of ulipristal acetate in cynomolgus monkeys. Regul Toxicol Pharmacol. 2013 Jun;66(1):6-12.

  [4]. Attardi BJ, et al. In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88.

  [5]. Ciarmela P, et al. Ulipristal acetate modulates the expression and functions of activin a in leiomyoma cells. Reprod Sci. 2014 Sep;21(9):1120-5.