CAS: 188968-51-6; 2-((2S,5R,8S,11S)-5-Benzyl-11-(3-Guanidinopropyl)-8-Isopropyl-7-Methyl-3,6,9,12,15-Pentaoxo-1,4,7,10,13-Pentaazacyclopentadecan-2-yl)Acetic Acid

该化合物是一种复杂的有机化合物,其特点是多周期结构和多种功能组的存在.这种化合物的特点是五色环戊二烷骨骼,有助于其独特的三维相容和潜在的生物活动.一个苯基和二氨甲基甲基氨基氨基氨基甲基胺动物的存在表明,该物质可能与生物目标产生有趣的互动,可能影响其药理特性.此外,乙酸功能组表明极溶剂具有溶解性,并可能在化合物的再活性中发挥作用.

结构式图片

上下游产品

CAS号199807-35-7 Cilengitide TFA | CAS号188969-00-8 Cyclo(L-arginyl...

合成工艺路线路线简述

    📜Cilengitide Hydrochloride置于ammonium Hydroxide体系中,用 水 用作溶剂,化学反应生成西仑吉肽
    参考文献:Pharmaceutical Composition Comprising Oligopeptides
    标题:Pharmaceutical Composition Comprising Oligopeptides
    摘要:本发明涉及一种寡肽的药物组合物,优选为环状寡肽,该组合物还包括一种或多种亲脂性和/或两性亲合性化合物,以水为主要成分的存在或不存在下,使用亲脂性和/或两性亲合性化合物制备所述寡肽的药物组合物,以及制备所述药物组合物的方法.

    海关参考信息

    专利信息


    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-12351573-B2
    优先权日:2019-05-09
    标 题:Compounds for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; CHENG KAI FAN
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

    专利号:US-2023159450-A1
    优先权日:2020-05-08
    标 题 :Dimers for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; ALTITI AHMAD
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

    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:US-2020354404-A1
    优先权日:2019-05-09
    标 题 :Peptidomimetic agents, synthesis and uses thereof
    发明人:AL-ABED YOUSEF
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

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    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: Kang HE, Seo Y, Kim Y, Kim J. Combined treatment of TKIs with Cilengitide overcomes afatinib-resistance in EGFR-mutated NSCLC cells. Mol Biol Rep. 2025 Dec 29;53(1):233. doi: 10.1007/s11033-025-11405-2. 54(7):597-606. doi: 10.1111/jop.70004. Epub 2025 Jul 1. 26(1):187. doi: 10.1186/s13058-024-01942-2.
    4: Guo DY, Chen ZH, Fu YF, Li YY, Chen MN, Wu JJ, Yuan ZD, Ye JX, Li X, Yuan FL. Corrigendum to "Cilengitide inhibits osteoclast adhesion through blocking the αvβ3-mediated FAK/Src signaling pathway" [Heliyon 9(7) (July 2023) e17841]. Heliyon. 2023 Nov 24;10(1):e22629. doi: 10.1016/j.heliyon.2023.e22629. Erratum for: Heliyon. 2023 Jun 29;9(7):e17841. doi: 10.1016/j.heliyon.2023.e17841.
    5: Flies CM, Friedrich M, Lohmann P, van Garderen KA, Smits M, Tonn JC, Weller M, Galldiks N, Snijders TJ. Treatment-associated imaging changes in newly diagnosed MGMT promoter-methylated glioblastoma undergoing chemoradiation with or without cilengitide. Neuro Oncol. 2024 May 3;26(5):902-910. doi: 10.1093/neuonc/noad247.

    合成参考文献


    参考文献:10.1007/s00259-002-0783-8
    摘要:Van de Wiele C, Oltenfreiter R, De Winter O, Signore A, Slegers G, Dierckx R. Tumour angiogenesis pathways: related clinical issues and implications for nuclear medicine imaging. European Journal of Nuclear Medicine and Molecular Imaging. 2002 Mar 22;29(5):699–709. doi: 10.1007/s00259-002-0783-8.
    参考文献:10.3892/or.19.4.1039
    摘要:Tentori L, Dorio A, Muzi A, Lacal P, Ruffini F, Navarra P, Graziani G. The integrin antagonist cilengitide increases the antitumor activity of temozolomide against malignant melanoma. Oncol Rep. 2008 Apr 01;(). doi: 10.3892/or.19.4.1039.
    参考文献:10.1186/bcr2835
    摘要:Clézardin P. Therapeutic targets for bone metastases in breast cancer. Breast Cancer Res. 2011 Apr 06;13(2):207.
    参考文献:10.4137/cmo.s7232
    摘要:Chamberlain MC. Bevacizumab for the treatment of recurrent glioblastoma. Clin Med Insights Oncol. 2011;5():117–29.
    参考文献:10.4414/smw.2011.13210
    摘要:Weller M. Novel diagnostic and therapeutic approaches to malignant glioma. Swiss Med Wkly. 2011;141():w13210. doi: 10.4414/smw.2011.13210.
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