6-amino-1H-pyrimidin-2-one;(2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 蝶啶及其衍生物
• 英文名称: 6-amino-1H-pyrimidin-2-one;(2S)-2-[[4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid
• 化学式: C24H27N11O6
• 分子量: 565.5
• InChiKey: CBKCJAUIDIJSDS-ZOWNYOTGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.38
• 重原子数：
  41
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  278
• 氢给体数：
  7
• 氢受体数：
  14

文献信息

• ANTIBODY-DRUG CONJUGATES CONTAINING AN ANTI-MESOTHELIN ANTIBODY AND USES THEREOF
  申请人：DEVELOPMENT CENTER FOR BIOTECHNOLOGY

  公开号：US20210386866A1

  公开（公告）日：2021-12-16

  The present disclosure provides an immunoconjugate includes an antibody comprising an antigen-binding fragment that specifically binds to an epitope in mesothelin, N-glycan binding domain and an N-glycan; a linker linking to the N-glycan; and a payload A and a payload B conjugated to the linker, respectively; wherein the payload A and the payload B are the same or different. A pharmaceutical composition comprises the immunoconjugate and a method for treating cancer are also provided in the disclosure.

  本公开提供了一种免疫结合物，包括抗体，其包括特异性结合于介质素中的表位的抗原结合片段、N-糖基结合结构域和N-糖基；连接到N-糖基的链接体；以及分别与链接体共轭的药物A和药物B；其中药物A和药物B可以相同或不同。本公开还提供了一种包含该免疫结合物的制药组合物以及治疗癌症的方法。
• Anti-VEGFR antibody and uses thereof
  申请人：DEVELOPMENT CENTER FOR BIOTECHNOLOGY

  公开号：US10138300B2

  公开（公告）日：2018-11-27

  The present invention relates to an antibody or antigen-binding fragment thereof that bind human vascular endothelial growth factor receptor 2 (VEGFR-2). The present invention also relates to a method for inhibiting VEGFR-2-mediated signaling in a subject in need, a method for treating diseases and/or disorders caused by or related to VEGFR-2 activity and/or signaling in a subject afflicted with the diseases and disorders, a method for treating tumor in a subject afflicted with the tumor, a method for inhibiting cell proliferation of endothelial cells in a subject in need, and a method for detecting human vascular endothelial growth factor receptor in a sample.

  本发明涉及一种结合人血管内皮生长因子受体2（VEGFR-2）的抗体或其抗原结合片段。本发明还涉及一种在有需要的受试者中抑制 VEGFR-2 介导的信号传导的方法，一种在患有疾病和失调的受试者中治疗由 VEGFR-2 活性和/或信号传导引起或与之相关的疾病和/或失调的方法，一种在患有肿瘤的受试者中治疗肿瘤的方法，一种在有需要的受试者中抑制内皮细胞的细胞增殖的方法，以及一种在样品中检测人血管内皮生长因子受体的方法。
• Processes for preparing glycoprotein-drug conjugates
  申请人：DEVELOPMENT CENTER FOR BIOTECHNOLOGY

  公开号：US11085062B2

  公开（公告）日：2021-08-10

  A process for modifying glycoproteins is provided. The invention also provides a process for producing glycoprotein-payload conjugates, as well as the conjugates produced thereby.

  本发明提供了一种修饰糖蛋白的工艺。本发明还提供了一种生产糖蛋白-载荷共轭物的工艺以及由此生产的共轭物。
• ADMINISTRATION OF AN ANTI-GCC ANTIBODY-DRUG CONJUGATE AND A DNA DAMAGING AGENT IN THE TREATMENT OF CANCER
  申请人：Millennium Pharmaceuticals, Inc.

  公开号：EP2961424A1

  公开（公告）日：2016-01-06
• COMPOUNDS AND COMPOSITIONS FOR IMAGING GCC-EXPRESSING CELLS
  申请人：Millennium Pharmaceuticals, Inc.

  公开号：EP3077407A1

  公开（公告）日：2016-10-12