(R)-3-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(2-bromophenyl)propanoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: (R)-3-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(2-bromophenyl)propanoic acid
• 英文别名: (3R)-3-(2-bromophenyl)-3-(9H-fluoren-9-ylmethoxycarbonylamino)propanoic acid
• 化学式: C₂₄H₂₀BrNO₄
• 分子量: 466.3
• InChiKey: DXTFQBWZFOPYGV-JOCHJYFZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  75.6
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Methods and Compositions for Improved F-18 Labeling of Proteins, Peptides and Other Molecules
  申请人：McBride William J.

  公开号：US20080170989A1

  公开（公告）日：2008-07-17

  The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen. Exemplary results show that F-18 labeled targetable conjugate peptides are stable in human serum at 37° C. for several hours, sufficient time to perform PET imaging analysis.

  本申请公开了合成和使用F-18标记分子的组成物和方法，例如在PET成像技术中使用。在特定实施例中，标记的分子可以是肽或蛋白质，尽管其他类型的分子，包括但不限于aptamer、寡核苷酸和核酸也可以被标记并用于这种成像研究。在优选实施例中，F-18标记可以通过形成金属配合物并将F-18金属配合物结合到螯合基团，例如DOTA、NOTA、DTPA、TETA或NETA，与靶向分子结合。在其他实施例中，金属可以首先与螯合基团结合，然后F-18与金属结合。在其他优选实施例中，F-18标记的分子可以包括可靶向的共轭物，可以与双特异性或多特异性抗体结合使用，以将F-18靶向表达在与疾病、医疗条件或病原体相关的细胞或组织上的抗原。示例结果表明，F-18标记的可靶向共轭肽在37℃的人血清中稳定数小时，足以进行PET成像分析。
• IMPROVED METHODS AND COMPOSITIONS FOR F-18 LABELING OF PROTEINS, PEPTIDES AND OTHER MOLECULES
  申请人：Immunomedics, Inc.

  公开号：EP2200657B1

  公开（公告）日：2015-12-02
• METHODS AND COMPOSITIONS FOR IMPROVED F-18 LABELING OF PROTEINS, PEPTIDES AND OTHER MOLECULES
  申请人：Immunomedics, Inc.

  公开号：EP2117604A2

  公开（公告）日：2009-11-18
• Methods and Compositions for F-18 Labeling of Proteins, Peptides and Other Molecules
  申请人：McBride William J.

  公开号：US20080253964A1

  公开（公告）日：2008-10-16

  The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen. Exemplary results show that F-18 labeled targetable conjugate peptides are stable in human serum at 37° C. for several hours, sufficient time to perform PET imaging analysis.
• US7563433B2
  申请人：——

  公开号：US7563433B2

  公开（公告）日：2009-07-21