4-Oxo-4-(2-thiophen-2-ylethylamino)butanoic acid

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 4-Oxo-4-(2-thiophen-2-ylethylamino)butanoic acid
• 化学式: C₁₀H₁₃NO₃S
• 分子量: 227.28
• InChiKey: FUSYKGHEWKQDDM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  94.6
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• CANCER TREATMENT COMPOSITION COMBINING ANTI-CD26 ANTIBODY AND OTHER ANTICANCER AGENT
  申请人：Y'S AC Co., Ltd.

  公开号：EP3348276A1

  公开（公告）日：2018-07-18

  An object of the present invention is to provide a novel highly safe method for treating mesothelioma. CD26 is overexpressed in mesothelioma and is considered to be highly safe. It has been revealed that the mesothelioma growth inhibitory effect of standard cisplatin-pemetrexed concomitant therapy is potentiated by combination with an anti-CD26 antibody. As a result of studying the effect of a humanized CD26 antibody and gemcitabine used concomitantly on the growth of a mesothelioma cell line, it has been found that a method for treating mesothelioma with a high therapeutic effect and excellent safety can be provided by the concomitant use of an anti-CD26 antibody and gemcitabine. As a result of conjugating an anti-CD26 antibody (YS110) with triptolide via a divalent cross-linking agent for concomitant therapy using the anti-CD26 antibody, a novel antibody-drug conjugate (Y-TR1) very highly effective for CD26-positive malignant mesothelioma cells has been successfully obtained.

  本发明的目的是提供一种治疗间皮瘤的高度安全的新方法。CD26 在间皮瘤中过度表达，被认为是高度安全的。研究发现，标准顺铂-培美曲塞联合疗法对间皮瘤生长的抑制作用通过与抗 CD26 抗体联合使用而得到增强。通过研究人源化 CD26 抗体和吉西他滨同时使用对间皮瘤细胞系生长的影响，发现同时使用抗 CD26 抗体和吉西他滨可以提供一种治疗间皮瘤的方法，该方法具有很高的治疗效果和极佳的安全性。通过一种二价交联剂将抗-CD26 抗体（YS110）与曲妥珠单抗共轭以同时使用抗-CD26 抗体进行治疗，成功地获得了一种对 CD26 阳性恶性间皮瘤细胞非常有效的新型抗体-药物共轭物（Y-TR1）。
• JPS606686A
  申请人：——

  公开号：JPS606686A

  公开（公告）日：1985-01-14