[(16E,18E)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] formate | 72816-07-0

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酰胺类
• 英文名称: [(16E,18E)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] formate
• CAS: 72816-07-0
• 化学式: C₂₉H₃₇ClN₂O₉
• 分子量: 593.074
• InChiKey: AMCBGGAVCLNTCA-IAGJPELUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  41
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  136
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• POTENT CONJUGATES AND HYDROPHILIC LINKERS
  申请人：SINGH Rajeeva

  公开号：US20120226026A1

  公开（公告）日：2012-09-06

  Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

  将药物与细胞结合剂结合的连接剂通过加入聚乙二醇间隔链被改变为亲水性连接剂。这种连接剂使得细胞结合剂-药物共轭物在多种癌细胞类型中的效力和功效惊人地提高，包括那些在细胞表面表达抗原数量较少或对治疗有抵抗性的癌细胞。同时，还提供了一种制备具有硫醚基和反应基的马替尼衍生物，该方法可以在基本上一步中将马替尼衍生物连接到细胞结合剂上。
• ANTI-ERBB2 ANTIBODY-DRUG CONJUGATE AND COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND USE THEREOF
  申请人：SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD.

  公开号：US20210252006A1

  公开（公告）日：2021-08-19

  Provided is a preparation method of an antibody-drug conjugate represented by Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof, or a solvate of the foregoing, wherein A, X, Y, L, D and a are as defined herein.