succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate | 85060-00-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate
• 英文别名: 1-[[4-(2,5-Dioxopyrrolidine-1-carbonyl)cyclohexyl]methyl]pyrrole-2,5-dione
• CAS: 85060-00-0
• 化学式: C₁₆H₁₈N₂O₅
• 分子量: 318.329
• InChiKey: SZRUATCSJOIIGX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  91.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate 、 盐酸多柔比星 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 12.0h， 以78%的产率得到doxorubicin
  参考文献：
  名称：

  [EN] BIOLOGICAL MATERIALS AND USES THEREOF
  [FR] MATÉRIELS BIOLOGIQUES ET LEURS UTILISATIONS

  摘要：

  该发明提供了包含治疗剂与载体分子偶联的化合物，最低偶联比为5:1；其中，载体分子是(i)抗体片段或其衍生物，或(ii)抗体模拟物或其衍生物；治疗剂偶联到赖氨酸氨基酸残基上；进一步，治疗剂不是光敏剂。还提供了关于这些化合物的用途、方法以及其制造过程。

  公开号：

  WO2016046574A1

文献信息

• Biological materials and uses thereof
  申请人：Antikor Biopharma Limited

  公开号：US11202837B2

  公开（公告）日：2021-12-21

  The invention provides compounds comprising a therapeutic agent coupled to a carrier molecule, with a minimum coupling ratio of 5:1; wherein the carrier molecule is (i) an antibody fragment or derivative thereof or (ii) an antibody mimetic or derivative thereof; and wherein the therapeutic agents are coupled onto a lysine amino acid residue; and further wherein the therapeutic agent is not a photosensitising agent. There is also provided uses, methods relating to such compounds, as well as processes for their manufacture.

  本发明提供了由治疗剂与载体分子偶联而成的化合物，最小偶联比为5:1；其中载体分子为(i)抗体片段或其衍生物或(ii)抗体模拟物或其衍生物；治疗剂偶联在赖氨酸氨基酸残基上；以及治疗剂不是光敏剂。此外，还提供了与此类化合物有关的用途、方法及其制造工艺。
• Maitotoxin-Photoactive Probe Binds to Membrane Proteins in Blood Cells
  作者：Keiichi Konoki、Michio Murata、Masaki Hashimoto、Kaori Honda、Kazuo Tachibana、Futoshi Hasegawa、Rie Tamate、Tohru Oishi

  DOI：10.3987/com-08-s(d)78

  日期：——

  The photoactive and biotinylating ligand was prepared from MTX and maleimide-conjugated Hatanaka reagent with use of Diels-Alder reaction. Blood cells were subjected to affinity labelling experiments using the ligand thus obtained. The labelled band on SDS-PAGE was replaced not by MTX but by brevetoxin B (PbTx2), which suggested the presence of binding proteins in blood cells. Screening of polyether compounds for MTX inhibitory activity using Ca(2+) flux assays in C6 cells disclosed that a synthetic fragment of the hydrophilic portion of MTX inhibited the MTX activity.
• CRAIG, ANDREW S.;HELPS, IAN M.;JANKOWSKI, KARL J.;PARKER, DAVID;BEELEY, N+, J. CHEM. SOC. CHEM. COMMUN.,(1989) N2, C. 794-796
  作者：CRAIG, ANDREW S.、HELPS, IAN M.、JANKOWSKI, KARL J.、PARKER, DAVID、BEELEY, N+

  DOI：——

  日期：——
• BIOLOGICAL MATERIALS AND USES THEREOF
  申请人：Antikor Biopharma Limited

  公开号：US20170360951A1

  公开（公告）日：2017-12-21

  The invention provides compounds comprising a therapeutic agent coupled to a carrier molecule, with a minimum coupling ratio of 5:1; wherein the carrier molecule is (i) an antibody fragment or derivative thereof or (ii) an antibody mimetic or derivative thereof; and wherein the therapeutic agents are coupled onto a lysine amino acid residue; and further wherein the therapeutic agent is not a photosensitising agent. There is also provided uses, methods relating to such compounds, as well as processes for their manufacture.
• [EN] BIOLOGICAL MATERIALS AND USES THEREOF<br/>[FR] MATÉRIELS BIOLOGIQUES ET LEURS UTILISATIONS
  申请人：ANTIKOR BIOPHARMA LTD

  公开号：WO2016046574A1

  公开（公告）日：2016-03-31

  The invention provides compounds comprising a therapeutic agent coupled to a carrier molecule, with a minimum coupling ratio of 5: 1; wherein the carrier molecule is (i) an antibody fragment or derivative thereof or (ii) an antibody mimetic or derivative thereof; and wherein the therapeutic agents are coupled onto a lysine amino acid residue; and further wherein the therapeutic agent is not a photosensitising agent. There is also provided uses, methods relating to such compounds, as well as processes for their manufacture.

  该发明提供了包含治疗剂与载体分子偶联的化合物，最低偶联比为5:1；其中，载体分子是(i)抗体片段或其衍生物，或(ii)抗体模拟物或其衍生物；治疗剂偶联到赖氨酸氨基酸残基上；进一步，治疗剂不是光敏剂。还提供了关于这些化合物的用途、方法以及其制造过程。