N-Me-D-Ala-maytansinol | 77714-98-8

• 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: N-Me-D-Ala-maytansinol
• 英文别名: 73Zat34esp；[(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] (2R)-2-(methylamino)propanoate
• CAS: 77714-98-8
• 化学式: C₃₂H₄₄ClN₃O₉
• 分子量: 650.169
• InChiKey: ANHBJISROJTYCJ-IQUQRBAYSA-N

物化性质

• 沸点：
  849.5±65.0 °C(Predicted)
• 密度：
  1.31±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  45
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  148
• 氢给体数：
  3
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  Fmoc-N-Me-D/L-Ala-maytansinol 在 哌啶 作用下， 以 乙腈 为溶剂， 反应 4.0h， 生成 N-deacetyl maytansine 、 N-Me-D-Ala-maytansinol
  参考文献：
  名称：

  [EN] COMPOUNDS AND METHODS FOR THE TREATMENT OF ERB B2/NEU POSITIVE DISEASES
  [FR] COMPOSÉS ET PROCÉDÉS PERMETTANT LE TRAITEMENT DE PATHOLOGIES ERB B2/NEU POSITIVES

  摘要：

  本文披露了与马替南素类药物结合的抗ERB B2/NEU抗体，用于靶向传递至疾病组织。提供了关于准备和使用这种药物结合物来治疗癌症中的ERB B2/NEU阳性细胞的方法。

  公开号：

  WO2014094527A1

文献信息

• Method for the preparation of maytansinoid esters
  申请人：Widdison C. Wayne

  公开号：US20060167245A1

  公开（公告）日：2006-07-27

  Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process of making a maytansinoid ester comprising forming an anion of maytansinol or a maytansinoid bearing a free C-3 hydroxyl moiety and reacting the anion with an activated carboxyl compound to thereby produce the maytansinoid ester.

  描述了用于制备和纯化美坦西酯类化合物的改进过程，特别是含有硫醇和二硫键的美坦西酯类化合物。在一个方面，该过程包括制备美坦西酯类化合物的过程，其中包括形成美坦西醇或带有游离C-3羟基的美坦西酯类化合物的阴离子，并将该阴离子与活化的羧基化合物反应，从而产生美坦西酯类化合物。
• [EN] AMINO ACID ACYLATION REAGENTS AND METHODS OF USING THE SAME<br/>[FR] RÉACTIFS D'ACYLATION D'ACIDES AMINÉS ET LEURS MÉTHODES D'UTILISATION
  申请人：REGENERON PHARMA

  公开号：WO2016149464A1

  公开（公告）日：2016-09-22

  Provided herein are compounds useful for appending amino acids to nucleophiles.

  本文提供了一些有用的化合物，用于将氨基酸附加到亲核试剂上。
• Compounds and methods for the treatment of TROP2 positive diseases
  申请人：BIO-THERA SOLUTIONS, LTD.

  公开号：US11192954B2

  公开（公告）日：2021-12-07

  The present invention generally relates to compounds comprising antibodies, antigen-binding fragments thereof, polypeptides, and immunoconjugates that bind to TROP2 (TACSTD2). The present invention also relates to methods of using such TROP2-binding molecules for diagnosing and treating diseases, such as malignancies.

  本发明一般涉及由抗体、其抗原结合片段、多肽和与 TROP2（TACSTD2）结合的免疫结合剂组成的化合物。本发明还涉及使用此类 TROP2 结合分子诊断和治疗疾病（如恶性肿瘤）的方法。
• COMPOUNDS AND METHODS FOR THE TREATMENT OF ERB B2/NEU POSITIVE DISEASES
  申请人：Bio-Thera Solutions, Ltd., Co.

  公开号：US20170258935A1

  公开（公告）日：2017-09-14

  Disclosed herein are anti-ERB B2/NEU antibodies conjugated with maytansinoid drugs for targeted delivery to disease tissues. Methods relating to the preparation and uses of such drug conjugates to treat ERB B2/NEU positive cells in cancers are provided.
• COMPOUNDS AND METHODS FOR THE TREATMENT OF TROP2 POSITIVE DISEASES
  申请人：BIO-THERA SOLUTIONS, LTD.

  公开号：US20190048095A1

  公开（公告）日：2019-02-14

  The present invention generally relates to compounds comprising antibodies, antigen-binding fragments thereof, polypeptides, and immunoconjugates that bind to TROP2 (TACSTD2). The present invention also relates to methods of using such TROP2-binding molecules for diagnosing and treating diseases, such as malignancies.