Calcein,AM

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: Calcein,AM
• 英文别名: acetyloxymethyl 2-[[2-(acetyloxymethoxy)-2-oxoethyl]-[[3',6'-diacetyloxy-5'-[[bis[2-(acetyloxymethoxy)-2-oxoethyl]amino]methyl]-3-oxospiro[2-benzofuran-1,9'-xanthene]-4'-yl]methyl]amino]acetate
• 化学式: C₄₆H₄₆N₂O₂₃
• 分子量: 994.9
• InChiKey: XKFSBWQWNMZWFA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  71
• 可旋转键数：
  32
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  305
• 氢给体数：
  0
• 氢受体数：
  25

反应信息

• 作为产物：
  描述：

  L-谷氨酰胺 、 葡萄糖 、 碳酸氢钠 、 Calcein-AM DMSO 生成 Calcein,AM
  参考文献：
  名称：

  Humanized Anti-Epiregulin Antibody, and Cancer Therapeutic Agent Comprising Said Antibody as Active Ingredient

  摘要：

  发明者们通过在人源化的EP27抗体的可变区序列中进行适当的氨基酸残基替换，成功生产了具有交叉物种反应性的抗Epiregulin抗体，包括猴子和人类，具有抑制化学降解的抗Epiregulin抗体，具有降低等电点的抗Epiregulin抗体，具有增加热变性中点温度的抗Epiregulin抗体，以及通过展示细胞毒性和中和人类表达Epiregulin的癌细胞的活性来抑制癌细胞生长的抗Epiregulin抗体，其聚集物的数量减少。

  公开号：

  US20150110793A1

文献信息

• Therapeutic Agent Comprising Humanized Anti-Epiregulin Antibody as Active Ingredient for Non-Small-Cell Lung Carcinoma Excluding Adenocarcinoma
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：US20160159919A1

  公开（公告）日：2016-06-09

  The present inventors successfully produced therapeutic agents for non-small cell lung cancer except adenocarcinoma, comprising as active ingredient an anti-Epiregulin antibody that shows cross-species reactivity between the human animal and cynomolgus which is a non-human animal, an anti-Epiregulin antibody with suppressed chemical degradation, an anti-Epiregulin antibody with reduced isoelectric point, an anti-Epiregulin antibody with increased midpoint temperature of thermal denaturation, or an anti-Epiregulin antibody with reduced amount of aggregates, generated by appropriately substituting amino acid residues in the variable-region sequences of a humanized EP27 antibody that inhibits cancer cell proliferation by exerting a cytotoxicity and a neutralizing activity against human Epiregulin-expressing cancer cells.

  本发明者成功地生产了治疗非腺癌非小细胞肺癌的治疗剂，其包含一种抗Epiregulin抗体作为活性成分，该抗体在人类动物和恒河猴等非人类动物之间显示跨物种反应性，或者是一种具有抑制化学降解的抗Epiregulin抗体，或者是一种具有降低等电点的抗Epiregulin抗体，或者是一种具有提高热变性中点温度的抗Epiregulin抗体，或者是一种具有减少聚集物量的抗Epiregulin抗体，通过在人源化的EP27抗体的可变区序列中适当替换氨基酸残基产生，该抗体通过对表达人类Epiregulin的癌细胞施加细胞毒性和中和活性来抑制癌细胞增殖。
• Humanized Anti-Epiregulin Antibody, and Cancer Therapeutic Agent Comprising Said Antibody as Active Ingredient
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：US20150110793A1

  公开（公告）日：2015-04-23

  The inventors successfully produced anti-Epiregulin antibodies showing cross-species reactivity between cynomolgus monkey (non-human animals) and human, anti-Epiregulin antibodies with suppressed chemical degradation, anti-Epiregulin antibodies with lowered isoelectric point, anti-Epiregulin antibodies with increased thermal denaturation midpoint temperature, and anti-Epiregulin antibodies with reduced amount of aggregate by performing appropriate amino acid residue substitutions in the variable-region sequences of the humanized EP27 antibody which inhibits growth of cancer cells by exhibiting cytotoxic activity and neutralizing activity against human Epiregulin-expressing cancer cells.

  发明者们通过在人源化的EP27抗体的可变区序列中进行适当的氨基酸残基替换，成功生产了具有交叉物种反应性的抗Epiregulin抗体，包括猴子和人类，具有抑制化学降解的抗Epiregulin抗体，具有降低等电点的抗Epiregulin抗体，具有增加热变性中点温度的抗Epiregulin抗体，以及通过展示细胞毒性和中和人类表达Epiregulin的癌细胞的活性来抑制癌细胞生长的抗Epiregulin抗体，其聚集物的数量减少。