CAS: 1404-15-5; Methyl (2R,3S,4R,5R,6R,11S,13S,14R)-4-(Dimethylamino)-3,5,8,10,13-Pentahydroxy-6,13-Dimethyl-9,16-Dioxo-11-(((2R,3R,4R,5S,6S)-3,4,5-Trimethoxy-4,6-Dimethyltetrahydro-2H-Pyran-2-yl)Oxy)-3,4,5,6,9,11,12,13,14,16-Decahydro-2H-2,6-Epoxytetraceno[1,2-B]Oxocine-14-Carboxylate

该化合物是一种炭疽抗生素,来源于鼻血管菌,以其强效抗肿瘤和抗菌特性著称,其结构具有独特的甜瓜糖味,增强了其DNA结合的亲和和和相互放大能力,从而有效地抑制了DNA和RNA合成.诺伽拉姆因素表现出了针对模范细菌和某些癌症细胞线的显著活动,特别是它能够诱发DNA链断裂并干扰二类异构体.它独特的行动机制及其结构特征使它成为肿瘤学和微生物学研究的宝贵化合物.然而,由于毒性很大,临床用途有限,促使人们不断研究各种衍生物,并改进了治疗指数.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-2012177593-A1
    优先权日:2009-07-20
    标 题 :Synthesis of dendrimer conjugates
    发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
    权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

    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-9879043-B1
    优先权日:2013-06-06
    标 题:Synthesis of non-natural cofactor analogs of S-adenosyl-L-methionine using methionine adenosyltransferase
    发明人:THORSON JON; HUBER TYLER; ZHANG JIANJUN; Singh Shanteri
    权利人:UNIV KENTUCKY RES FOUND
    摘要:The present disclosure relates to the synthesis of non-natural analogs of S-adenosyl-L-methionine (SAM) and/or of Se-adenosyl-L-methionine (SeAM) by reacting a methionine analog and adenosine triphosphate (ATP) in the presence of at least one methionine adenosyltransferase (MAT), and to use thereof with downstream SAM and/or SeAM utilizing enzymes. The non-natural analogs of SAM and/or SeAM have the general formula: n nwhere X is S or Se, and R 1 is an alkyl group.

    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.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Klymyshin D, Stephanyshyn O, Fedorenko V. [THE ROLE OF (p)ppGpp MOLECULES IN FORMATION OF "STRICT RESPONSE" IN BACTERIA AND BIOSYNTHESIS OF ANTIBIOTICS AND MORPHOLOGICAL DIFFERENTIATION IN ACTINOMYCETES]. Tsitol Genet. 2016 Mar-Apr;50(2):65-74. Review. Russian. Review. Review. Japanese. Review. Review. Japanese. Review. Japanese. Review. Review. Review. Review. Review.
    12: Wadler S, Fuks JZ, Wiernik PH. Phase I and II agents in cancer therapy: I. Anthracyclines and related compounds. J Clin Pharmacol. 1986 Sep-Oct;26(7):491-509. Review. Review. Review. Review.

    合成参考文献


    摘要:Advances in Teratology., 3(181), 1968
    摘要:Progress Report Submitted to the National Cancer Insitute by Piason Research Institute., -(192), 1966
    参考文献:10.1006/jmbi.1999.2903
    摘要:Williams HEL, Searle MS. Structure, dynamics and hydration of the nogalamycin-d(ATGCAT) 2 complex determined by NMR and molecular dynamics simulations in solution 1 1Edited by I. Tinoco. Journal of Molecular Biology. 1999 Jan;290(3):699–716. doi: 10.1006/jmbi.1999.2903.
    参考文献:10.1107/s090744490400705x
    摘要:Sultana A, Kallio P, Jansson A, Niemi J, Mäntsälä P, Schneider G. Crystallization and preliminary crystallographic data of SnoaL, a polyketide cyclase in nogalamycin biosynthesis. Acta Crystallogr D Biol Crystallogr. 2004 Jun;60(Pt 6):1118–20. doi: 10.1107/s090744490400705x.
    参考文献:10.1021/bi00363a026
    摘要:Fox KR, Waring MJ. Nucleotide sequence binding preferences of nogalamycin investigated by DNase I footprinting. Biochemistry. 1986 Jul 29;25(15):4349–56. doi: 10.1021/bi00363a026.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知