maytanbutine | 38997-10-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酰胺类
• 英文名称: maytanbutine
• 英文别名: [(1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[methyl(2-methylpropanoyl)amino]propanoate
• CAS: 38997-10-3；70774-06-0
• 化学式: C₃₆H₅₀ClN₃O₁₀
• 分子量: 720.26
• InChiKey: RJIVUFYDGYNSNE-IZKDVACGSA-N

物化性质

• 沸点：
  900.9±65.0 °C(Predicted)
• 密度：
  1.29±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  50
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  157
• 氢给体数：
  2
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  maytanbutine 在 吡啶 、 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 21.0h， 生成 Maytansinol-3-bromacetat (12)
  参考文献：
  名称：

  天然和半合成美登木素生物碱中抗白血病活性的结构要求。

  摘要：

  为了确定新的ansa大环内酯所表现出的显着的抗白血病，细胞毒性，抗微管蛋白和抗有丝分裂活性的结构要求，合成了美登素（1），四个新的C-3酯和六个新的C-9醚同系物。分析了这些化合物的生物学活性，并将其与先前报道的天然存在的美登木素生物碱的活性进行了比较。从数据可以明显看出，C-3酯的存在对于显着的活性是必要的，并且酯基的变化不伴随活性的显着变化。然而，如美登醇（7），蛋黄素（8），去甲蛋黄素（9）和蛋氨酸（10）中那样，酯基的消除导致生物活性显着降低。通过醚化作用阻断C-9羧酰胺显着降低了抗白血病和细胞毒性活性，并稍微降低了抗微管蛋白活性，但对海胆卵的抗有丝分裂活性影响相对较小。因此，C-9处的游离羧酰胺对于最佳活性是有利的。

  DOI：

  10.1021/jm00199a006

文献信息

• [EN] DRUG-PROTEIN CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENT-PROTÉINE
  申请人：POLYTHERICS LTD

  公开号：WO2014064423A1

  公开（公告）日：2014-05-01

  Specific conjugates containing auristatins and a binding protein or peptide, and processes for making them, are described. The conjugates use specific linker technology which gives advantages over known antibody-drug conjugates. Also described are specific conjugates of drugs and a binding protein or peptide in which more than one copy of the drug is present.

  包含奥利司他汀和结合蛋白或肽的特定共轭物以及制备它们的过程被描述。这些共轭物使用特定的连接技术，相比已知的抗体药物共轭物具有优势。还描述了药物和结合蛋白或肽的特定共轭物，其中药物的副本超过一个。
• DRUG-PROTEIN CONJUGATES
  申请人：POLYTHERICS LIMITED

  公开号：US20150290342A1

  公开（公告）日：2015-10-15

  Specific conjugates containing auristatins and a binding protein or peptide, and processes for making them, are described. The conjugates use specific linker technology which gives advantages over known antibody-drug conjugates. Also described are specific conjugates of drugs and a binding protein or peptide in which more than one copy of the drug is present.

  本发明涉及含有奥利司他汀和结合蛋白或肽的特定共轭物，以及制备它们的过程。这些共轭物使用特定的连接技术，比已知的抗体药物共轭物具有优势。本发明还描述了药物和结合蛋白或肽的特定共轭物，其中药物的副本超过一个。
• Anti-CD123 antibodies and conjugates and derivatives thereof
  申请人：IMMUNOGEN, INC.

  公开号：US10875925B2

  公开（公告）日：2020-12-29

  The present invention generally relates to antibodies, antigen-binding fragments thereof, polypeptides, and immunoconjugates that bind to CD123 antigen (the α chain of the interleukine 3 receptor, or IL-3Rα). The present invention also relates to methods of using such CD123-binding molecules for diagnosing and treating diseases, such as B-cell malignancies.

  本发明一般涉及与 CD123 抗原（白细胞介素 3 受体或 IL-3Rα 的 α 链）结合的抗体、其抗原结合片段、多肽和免疫结合剂。本发明还涉及使用此类 CD123 结合分子诊断和治疗疾病（如 B 细胞恶性肿瘤）的方法。
• ANTIBODIES, ANTIBODY DRUG CONJUGATES AND METHODS OF USE
  申请人：GAMAMABS PHARMA

  公开号：US20170035903A1

  公开（公告）日：2017-02-09

  This invention relates to antibody drug conjugates (ADC), antibody conjugates (AC) and novel antibodies. Particularly, the ADC, AC and antibodies disclosed herein specifically bind to the human anti-Müllerian hormone type II receptor (AMHR-II) and can be used to treat and/or identify AMHR-II expressing cancers, such as prostate cancer, breast cancer and gynecologic cancers expressing AMHR-II, such as ovarian cancer, in particular metastatic ovarian cancer, serous cancer, hypernephroma, endometrioid, colloidal epithelium, prostate cancer, germ cell cancer, endometrial cancer, mixed Müllerian malignant tumor of the uterus, leiomyosarcoma, or endometrial stromal sarcoma.
• ANTI-CD123 ANTIBODIES AND CONJUGATES AND DERIVATIVES THEREOF
  申请人：IMMUNOGEN, INC.

  公开号：US20200239580A1

  公开（公告）日：2020-07-30

  The present invention generally relates to antibodies, antigen-binding fragments thereof, polypeptides, and immunoconjugates that bind to CD123 antigen (the α chain of the interleukine 3 receptor, or IL-3Rα). The present invention also relates to methods of using such CD123-binding molecules for diagnosing and treating diseases, such as B-cell malignancies.