718612-62-5

• 常用中文名：伊立替康-D10盐酸盐
• 常用英文名：Irinotecan-d10 (hydrochloride)
• CAS号：718612-62-5
• 分子式：C₃₃H₂₉D₁₀ClN₄O₆
• 分子量：633.201
• 相关类别： 信号通路 自噬 自噬
• 发布时间：2021-06-01 20:35:13
• 更新时间：2024-01-16 04:49:40
• 伊立替康-d10(+)-伊立替康-d10)盐酸盐是氘标记的伊立替康。伊立替康(+)-伊立替康)是一种拓扑异构酶I抑制剂,通过与拓扑异构酶I-DNA复合物结合来阻止DNA链的释放[1][2]。

名称

• 中文名: 伊立替康-D10盐酸盐
• 英文名: Irinotecan-d10 (hydrochloride)
• 英文别名: [1,4'-Bipiperidine-2,2,3,3,4,4,5,5,6,6-d10]-1'-carboxylic acid, (4S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester, hydrochloride (1 :1); (4S)-4,11-Diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl (2,2,3,3,4,4,5,5,6,6-2H10)-1,4'-bipiperidine-1'-carboxylate hydrochloride (1:1); Irinotecan-d10 (hydrochloride)

物化性质

• 分子式: C₃₃H₂₉D₁₀ClN₄O₆
• 分子量: 633.201
• 精确质量: 632.318604

生物活性

• 描述: 伊立替康-d10(+)-伊立替康-d10)盐酸盐是氘标记的伊立替康。伊立替康(+)-伊立替康)是一种拓扑异构酶I抑制剂,通过与拓扑异构酶I-DNA复合物结合来阻止DNA链的释放[1][2]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶
  信号通路 >> 自噬 >> 自噬
• 体外研究: 氢、碳和其他元素的稳定重同位素已被纳入药物分子,主要作为药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。
• 参考文献:

  [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

  [2]. Morales C, et al. Antitumoral effect of irinotecan (CPT-11) on an experimental model of malignant neuroectodermal tumor. J Neurooncol. 2002 Feb;56(3):219-26.

  [3]. Pavillard V, et al. Determinants of the cytotoxicity of irinotecan in two human colorectal tumor cell lines. Cancer Chemother Pharmacol. 2002 Apr;49(4):329-35. Epub 2002 Jan 30.

  [4]. Allegrini G, et al. Thrombospondin-1 plus irinotecan: a novel antiangiogenic-chemotherapeutic combination that inhibits the growth of advanced human colon tumor xenografts in mice. Cancer Chemother Pharmacol. 2004 Mar;53(3):261-6. Epub 2003 Dec 5.

  [5]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116.

  [6]. Huang MY, et al. Chemotherapeutic agent CPT-11 eliminates peritoneal resident macrophages by inducing apoptosis. Apoptosis. 2016 Feb;21(2):130-42.