乙二醇-双(丁二酸 N-羟基琥珀酰亚胺酯) | 70539-42-3

• 物质功能分类: 催化剂及助剂 - 聚乙二醇衍生物
• 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
• 中文名称: 乙二醇-双(丁二酸 N-羟基琥珀酰亚胺酯)
• 中文别名: 二(N-琥珀酰亚胺)乙二醇二琥珀酸酯；乙二醇-双(丁二酸N-羟基琥珀酰亚胺酯)；乙二醇-双(琥珀酸N-羟基琥珀酰亚胺酯)；二(N-琥珀酰亚胺)乙烯乙二醇二琥珀酸酯
• 英文名称: ethylene glycol bis(succinimidyl succinate)
• 英文别名: EGS；4-O-(2,5-dioxopyrrolidin-1-yl) 1-O-[2-[4-(2,5-dioxopyrrolidin-1-yl)oxy-4-oxobutanoyl]oxyethyl] butanedioate
• CAS: 70539-42-3
• 化学式: C₁₈H₂₀N₂O₁₂
• mdl: MFCD00049057
• 分子量: 456.363
• InChiKey: QLHLYJHNOCILIT-UHFFFAOYSA-N

物化性质

• 沸点：
  603.4±65.0 °C(Predicted)
• 密度：
  1.52±0.1 g/cm3(Predicted)
• 溶解度：
  醋酸：水（1:1）：≤50mg/mL
• 稳定性/保质期：

  远离氧化物。

计算性质

• 辛醇/水分配系数(LogP)：
  -2.3
• 重原子数：
  32
• 可旋转键数：
  15
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.555
• 拓扑面积：
  180
• 氢给体数：
  0
• 氢受体数：
  12

安全信息

• WGK Germany：
  3
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335
• 储存条件：
  存放在密封容器内，并置于阴凉、干燥处。请将储存地点远离氧化剂。另外，该物品应在2-8 ºC的条件下保存。

制备方法与用途

用途

这是一种兼具双重功能且可裂解的交联剂，主要通过在pH值为6.5至8.5范围内（尤其是7.5时）形成的酰胺键，将含有伯胺基团的分子进行偶联。

反应信息

• 作为反应物：
  描述：

  两性霉素B 、 乙二醇-双(丁二酸 N-羟基琥珀酰亚胺酯) 在 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  Amphotericin B Covalent Dimers Forming Sterol-Dependent Ion-Permeable Membrane Channels

  摘要：

  Polyenemacrolides such as amphotericin B (AmB) were thought to assemble together and form an ion channel across plasma membranes. Their antimicrobial activity has been accounted for by this assemblage, whose stability and activity are dependent on sterol constituents of lipid bilayer membranes. The structure of this channel-like assemblage formed in biomembranes has been a target of extensive investigations for a long time. For the first step to this goal, we prepared several AmB dimers with various linkers and tested for their channel-forming activity. Among these, AmB dimers that bore an aminoalkyl-dicarboxylate tether covalently linked between amino groups of AmB showed potent hemolytic activity. Furthermore, K+ influx actions monitored by measuring the pH of the liposome lumen by 31P NMR revealed that the dimers formed the molecular assemblage similar to that of AmB in phospholipid membrane. Judging from changes in 31P NMR spectra, the dimers appeared to induce "all-or-none"-type ion flux across the liposome membrane in the presence of ergosterol, which suggested that the ion channel formed by ergosterol/dimer is similar to that of AmB. With these data in hand, we are now trying to elucidate the structure of the ion-channel complex by making the labeled conjugates of AmB for NMR measurements.

  DOI：

  10.1021/ja012026b

文献信息

• Anti-Claudin 3 Monoclonal Antibody and Treatment and Diagnosis of Cancer Using the Same
  申请人：YOSHIDA Kenji

  公开号：US20100111852A1

  公开（公告）日：2010-05-06

  Monoclonal antibodies that bind specifically to Claudin 3 expressed on cell surface are provided. The antibodies of the present invention are useful for diagnosis of cancers that have enhanced expression of Claudin 3, such as ovarian cancer, prostate cancer, breast cancer, uterine cancer, liver cancer, lung cancer, pancreatic cancer, stomach cancer, bladder cancer, and colon cancer. The present invention provides monoclonal antibodies showing cytotoxic effects against cells of these cancers. Methods for inducing cell injury in Claudin 3-expressing cells and methods for suppressing proliferation of Claudin 3-expressing cells by contacting Claudin 3-expressing cells with a Claudin 3-binding antibody are disclosed. The present application also discloses methods for diagnosis or treatment of cancers.

  提供了特异性结合于细胞表面表达的Claudin 3的单克隆抗体。本发明的抗体对于具有增强Claudin 3表达的癌症的诊断是有用的，如卵巢癌、前列腺癌、乳腺癌、子宫癌、肝癌、肺癌、胰腺癌、胃癌、膀胱癌和结肠癌。本发明提供了对这些癌症细胞具有细胞毒作用的单克隆抗体。公开了诱导Claudin 3表达细胞受损的方法以及通过与Claudin 3结合抗体接触Claudin 3表达细胞来抑制Claudin 3表达细胞增殖的方法。本申请还公开了癌症的诊断或治疗方法。
• KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
  申请人：Imago Biosciences, Inc.

  公开号：US20160237043A1

  公开（公告）日：2016-08-18

  Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

  本文披露了新化合物和组合物，以及它们作为药物治疗疾病的应用。还提供了抑制KDM1A的方法，增加γ球蛋白基因表达的方法，以及诱导人类或动物主体中癌细胞分化的方法，用于治疗急性髓性白血病等疾病。
• [EN] KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE<br/>[FR] INHIBITEURS DE KDM1A POUR LE TRAITEMENT D'UNE MALADIE
  申请人：IMAGO BIOSCIENCES

  公开号：WO2014164867A1

  公开（公告）日：2014-10-09

  Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, and methods of increasing gamma globin gene expression in a human or animal subject are also provided for the treatment diseases such as sickle cell disease.

  本文披露了新化合物和组合物，以及它们作为药物治疗疾病的应用。还提供了抑制KDMIA的方法，以及增加人类或动物主体中γ球蛋白基因表达的方法，用于治疗镰状细胞病等疾病。
• ANTIBODY-ALK5 INHIBITOR CONJUGATES AND THEIR USES
  申请人：Synthis, LLC

  公开号：US20200147234A1

  公开（公告）日：2020-05-14

  The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.

  本公开涉及包含ALK5抑制剂的抗体药物偶联物及其用途。
• [EN] ANTIB0DY-ALK5 INHIBITOR CONJUGATES AND THEIR USES<br/>[FR] CONJUGUÉS D'ANTICORPS-INHIBITEUR DE ALK5 ET LEURS UTILISATIONS
  申请人：SYNTHIS LLC

  公开号：WO2020256751A1

  公开（公告）日：2020-12-24

  The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.

  本公开涉及包含ALK5抑制剂的抗体药物偶联物及其用途。