MAL-dPEG₂-TFP | 1431291-44-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚酯
• 英文名称: MAL-dPEG₂-TFP
• 英文别名: MaI-PEG2-TFP；Mal-amido-PEG2-TFP ester；(2,3,5,6-tetrafluorophenyl) 3-[2-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxy]propanoate
• CAS: 1431291-44-9
• 化学式: C₂₀H₂₀F₄N₂O₇
• 分子量: 476.382
• InChiKey: HHXSYLTYQVHXMA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  33
• 可旋转键数：
  14
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  111
• 氢给体数：
  1
• 氢受体数：
  11

反应信息

• 作为反应物：
  描述：

  tert-butyl (S)-18,22-diamino-17-oxo-4,7,10,13-tetraoxa-16-azadocosanoate 、 MAL-dPEG₂-TFP 在 2,6-二甲基吡啶 作用下， 以 二氯甲烷 为溶剂， 以51.7%的产率得到MAL-dPEG₂-Lys(MAL-dPEG₂)-dPEG₄-TBE
  参考文献：
  名称：

  Branched Discreet PEG Constructs

  摘要：

  揭示了一般的和“基本纯净”的分支离散聚乙二醇构建物，可用于连接各种生物活性基团，例如，偏好定位器，以及生物制剂如酶，用于诊断，例如成像，治疗，治疗诊断学和特定于其他应用的基团。在其最简单的中间状态中，分支离散聚乙二醇构建物在一端由一种化学反应性基团“A”终止，该基团与创建“A”的生物材料发生反应，该生物材料是一种生物反应性基团，通过连接到至少两个dPEG含链的分支核心（BC）结束，这些链由实线表示，具有端基团，可以是带电的、非反应性的或可反应的基团，并含有约2至64个dPEG残基。

  公开号：

  US20130052130A1

文献信息

• [EN] LINKERS FOR IMPROVING THE STABILITY OF BIOCONJUGATES AND THE SELECTIVITY OF PAYLOAD RELEASE<br/>[FR] LIEURS PERMETTANT D'AMÉLIORER LA STABILITÉ DE BIOCONJUGUÉS ET LA SÉLECTIVITÉ DE LIBÉRATION DE CHARGE UTILE
  申请人：EQIP LLC

  公开号：WO2022165335A1

  公开（公告）日：2022-08-04

  Disclosed herein are linker architectures for conjugates that do not rely on the SAR of the cleavable trigger or the large steric bulk of a closely positioned antibody to alter payload release. These linkers are expected to reduce off-target payload release facilitated by extracellular cathepsins, and may also be applicable to conjugates of antibody fragments that lack the steric protection from a full antibody. In addition, the linkers disclosed herein are expected to provide more selective intracellular payload release. Thus, these linkers can function synergistically with the targeting vector to confer differential payload release rates in vivo that improve the selectivity of intracellular payload release and reduce off target toxicity.

  本文揭示了一种连接体架构，用于结合物，不依赖于可切割触发器的SAR或临近抗体的大立体体积来改变荷载释放。预计这些连接剂将减少由细胞外半胱天蛋白酶促进的非靶向荷载释放，并且也适用于缺乏完整抗体的抗体片段的结合物。此外，本文揭示的连接剂预计提供更有选择性的细胞内荷载释放。因此，这些连接剂可以与靶向载体协同作用，以在体内提供不同的荷载释放速率，从而提高细胞内荷载释放的选择性并减少非靶向毒性。
• BRANCHED DISCRETE PEG CONSTRUCTS
  申请人：Quanta Biodesign, Ltd.

  公开号：EP2750681B1

  公开（公告）日：2020-05-27
• Branched Discrete PEG Constructs
  申请人：Davis Paul D.

  公开号：US20170313656A1

  公开（公告）日：2017-11-02

  Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.
• COMPOUNDS COMPRISING A LINKER FOR INCREASING TRANSCYCLOOCTENE STABILITY
  申请人：Tagworks Pharmaceuticals B.V.

  公开号：US20210308207A1

  公开（公告）日：2021-10-07

  Disclosed are compounds having a linker for increasing trans-cyclooctene stability. The linker of the invention is a three-arm linker. In some embodiments, one arm of the linker is attached to a trans-cyclooctene moiety, another arm is attached to a compound selected from the group consisting of antibodies, proteins, peptides, and peptoids, and the third arm extends into the solution.
• [EN] TARGETING CONJUGATES COMPRISING TARGETING MOIETY BINDING FRAGMENTS AND USES THEREOF<br/>[FR] CONJUGUÉS DE CIBLAGE COMPRENANT DES FRAGMENTS DE LIAISON À UNE FRACTION DE CIBLAGE ET LEURS UTILISATIONS
  申请人：[en]SHANGHAI ALLYGEN BIOLOGICS CO., LTD.

  公开号：WO2022178753A1

  公开（公告）日：2022-09-01

  Provided are targeting conjugates comprising a targeting moiety and an effector molecule, wherein the effector molecule is attached to the targeting moiety via a targeting moiety binding fragment (TBF), wherein the effector molecule can be released from the targeting conjugate via cleavage. Also provided are compositions and methods of treatment or diagnosis using the targeting conjugates.