4-({2-[1-Acetoxy-4-methyl-3-((3-methyl-butyryloxymethyl)-{3-methyl-2-[(1-methyl-piperidine-2-carbonyl)-amino]-pentanoyl}-amino)-pentyl]-thiazole-4-carbonyl}-amino)-5-(4-hydroxy-phenyl)-2-methyl-pentanoic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4-({2-[1-Acetoxy-4-methyl-3-((3-methyl-butyryloxymethyl)-{3-methyl-2-[(1-methyl-piperidine-2-carbonyl)-amino]-pentanoyl}-amino)-pentyl]-thiazole-4-carbonyl}-amino)-5-(4-hydroxy-phenyl)-2-methyl-pentanoic acid
• 英文别名: TubA；4-[[2-[1-acetyloxy-4-methyl-3-[3-methylbutanoyloxymethyl-[3-methyl-2-[(1-methylpiperidine-2-carbonyl)amino]pentanoyl]amino]pentyl]-1,3-thiazole-4-carbonyl]amino]-5-(4-hydroxyphenyl)-2-methylpentanoic acid
• 化学式: C₄₃H₆₅N₅O₁₀S
• 分子量: 844.083
• InChiKey: IBEDDHUHZBDXGB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  59
• 可旋转键数：
  24
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  233
• 氢给体数：
  4
• 氢受体数：
  13

反应信息

• 作为反应物：
  描述：

  对苯二胺 、 4-({2-[1-Acetoxy-4-methyl-3-((3-methyl-butyryloxymethyl)-{3-methyl-2-[(1-methyl-piperidine-2-carbonyl)-amino]-pentanoyl}-amino)-pentyl]-thiazole-4-carbonyl}-amino)-5-(4-hydroxy-phenyl)-2-methyl-pentanoic acid 生成 [[1-Acetyloxy-1-[4-[[5-(4-aminoanilino)-1-(4-hydroxyphenyl)-4-methyl-5-oxopentan-2-yl]carbamoyl]-1,3-thiazol-2-yl]-4-methylpentan-3-yl]-[3-methyl-2-[(1-methylpiperidine-2-carbonyl)amino]pentanoyl]amino]methyl 3-methylbutanoate
  参考文献：
  名称：

  [EN] SELF-IMMOLATIVE LINKERS AND DRUG CONJUGATES
  [FR] BRAS DE LIAISON CHIMIQUES ET CONJUGUES ASSOCIES

  摘要：

  公开号：

  WO2005112919A3

文献信息

• CHEMICAL LINKERS AND CONJUGATES THEREOF
  申请人：Boyd Sharon E.

  公开号：US20100092496A1

  公开（公告）日：2010-04-15

  The present disclosure provides drug-ligand conjugates that are potent cytotoxins, wherein the drug is linked to the ligand through either a peptidyl, hydrazine, or disulfide linker. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

  本公开提供了药物-配体共轭物，其具有强效的细胞毒性，其中药物通过肽基、肼基或二硫键连接到配体上。该公开还涉及含有药物-配体共轭物的组合物，以及使用它们的治疗方法。
• Macrophage stimulating protein receptor (or RON—recepteur d'Origine Nantais) antibodies and uses thereof
  申请人：AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

  公开号：US11225515B2

  公开（公告）日：2022-01-18

  Disclosed are monoclonal antibodies that bind specifically to macrophage stimulating protein receptor (or RON—Recepteur d' Origine Nantais). Also provided are the chimeric antigen receptors, bispecific antibodies, bivalent antibodies and biTE thereof, as well as pharmaceutical compositions and uses of said antibodies for the treatment of cancer and fibrosis and an ex vivo method of evaluating the status of a cancer patient using said antibodies. In particular, two monoclonal antibodies, 7G8 and 6D4, demonstrating good therapeutic efficacy in inhibiting tumour growth in human xenograft mice models and sensitivity in human xenograft mouse tumour imaging models are provided.

  本研究公开了与巨噬细胞刺激蛋白受体（或 RON-Recepteur d' Origine Nantais）特异性结合的单克隆抗体。此外，还提供了嵌合抗原受体、双特异性抗体、二价抗体及其双TE，以及上述抗体用于治疗癌症和纤维化的药物组合物和用途，以及使用上述抗体评估癌症患者状况的体外方法。特别是提供了两种单克隆抗体 7G8 和 6D4，这两种抗体在人类异种移植小鼠模型中抑制肿瘤生长方面表现出良好的疗效，在人类异种移植小鼠肿瘤成像模型中表现出敏感性。
• MACROPHAGE STIMULATING PROTEIN RECEPTOR (OR RON - RECEPTEUR D' ORIGINE NANTAIS) ANTIBODIES AND USES THEREOF
  申请人：Agency for Science, Technology and Research

  公开号：EP3504244A1

  公开（公告）日：2019-07-03
• Antibody-Drug Conjugates and Methods of Use
  申请人：Boyd Sharon Elaine

  公开号：US20080279868A1

  公开（公告）日：2008-11-13

  The present disclosure provides antibody-drug conjugates that are potent cytotoxins, wherein the drug is linked to the antibody through a linker. The disclosure is also directed to compositions containing the antibody-drug conjugates, and to methods of treatment using them.
• US7691962B2
  申请人：——

  公开号：US7691962B2

  公开（公告）日：2010-04-06