CAS: 576-68-1; Mannomustine

该化合物是一种化学化合物,属于烷基制剂类别,特别是芥子的衍生物,其特点是能够与DNA形成共价联系,导致DNA复制和转录过程的交叉联系和随后的中断.这一行动机制使Mannomustine可以用于癌症治疗,特别是治疗某些种类的肿瘤.该化合物一般是白到白的,在各种有机溶剂中可溶解.其化学结构包括一种有助于其再活性和生物活动的芥子细胞.正如许多烷基制剂一样,Mannomustine可能表现出细胞毒性效应,其使用与潜在副作用有关,包括乳房压抑和其他毒性.由于其药理学特性,人乳素对医药化学和肿瘤研究感兴趣,尽管其临床应用可能受到安全和功效因素的限制.

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23323-37-7 2227486-62-4 35564-86-4

MSDS等安全信息

    合成工艺路线路线简述

      📜1,6-Bis-Aziridin-1-Yl-O3,O4-Isopropylidene-1,6-Dideoxy-D-Mannitol置于盐酸,甲醇,水体系中,化学反应生成 甘露醇氮芥
      参考文献:Vargha Et Al.,Journal Of The Chemical Society,1957,P. 805,809
      标题:Vargha Et Al.,Journal Of The Chemical Society,1957,P. 805,809

      海关参考信息

      专利信息


      专利号:US-10925977-B2
      优先权日:2006-10-05
      标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
      发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
      权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
      摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

      专利号:US-12391691-B2
      优先权日:2018-11-16
      标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
      发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
      权利人:AMGEN INC
      摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

      专利号:US-2025206736-A1
      优先权日:2019-11-14
      标题 :Synthesis of kras g12c inhibitor compound
      发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
      权利人:AMGEN INC
      摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

      专利号:WO-2017100796-A1
      优先权日:2015-12-11
      标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
      发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
      权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
      摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.

      专利号:US-2017283878-A1
      优先权日:2015-12-11
      标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
      发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
      权利人:ACADEMIA SINICA
      摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

      专利号:US-10342858-B2
      优先权日:2015-01-24
      标题 :Glycan conjugates and methods of use thereof
      发明人:WONG CHI-HUEY; WU CHUNG-YI
      权利人:ACADEMIA SINICA
      摘要:The present disclosure is directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA3/SSEA4/GloboH associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3/SSEA4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions.

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      主要参考文献

      1. BARLOW AM, LEEMING JT, WILKINSON JF. Mannomustine in treatment of leukaemias, polycythaemia, and malignant disorders. Br Med J. 1959 Aug 22;2(5146):208-13. doi: 10.1136/bmj.2.5146.208.

      合成参考文献


      摘要:Arzneimittel-Forschung. Drug Research., 11(143), 1961 []
      摘要:Arzneimittel-Forschung. Drug Research., 20(1467), 1970 []
      摘要:Kholodnyi MD, Mindlin SS. [The hypoplastic state of hematopoiesis following chemotherapy with alkylating compounds]. Vopr Onkol. 1969;15(8):27–32.
      摘要:Gergely P, Szabó G, Szegedi G, Fekete B, Petrányi G. In-vitro sensitivity to cytostatics in chronic myeloid leukaemia. Acta Med Acad Sci Hung. 1973;29(3):285–9.
      参考文献:10.1007/bf01256068
      摘要:Scherf HR, Karsten C, Krüger C. [Animal experimental studies on the immunosuppressive effect of cytostatic agents]. Langenbecks Arch Chir. 1969;325():1028–33. doi: 10.1007/bf01256068.
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