CAS: 57576-44-0; Aclacinomycin A

该化合物是一种炭疽抗生素,主要用作抗乳胶剂,主要用作抗乳胶剂,主要通过脱氧核糖核糖核酸和抑制二氧化异构体酶表现出强大的细胞毒性活动,导致DNA复制和转录中断.与其他炭疽菌相比,氨基丁二醇表明其心毒性降低,这是长期治疗应用的一大优势.其机制还包括产生反应性氧物种,有助于肿瘤细胞的血压化.该化合物在治疗急性流血性白血病(AML)和其他血解恶性肿瘤方面特别有效.氨基乙醇的有利药用植物基因特征,包括快速细胞吸收和保留,提高了其治疗效率,同时将系统毒性降到最低.其临床用途凸显了其作为宝贵的取水器选择的作用.

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(+)-aklavinone 3',3'-didesmethyl-aclarubicin (+)-aklavinone 3,5,5-trimethyl-2-oxomorpholine 5,6-dihydro-3,5,5-trimethyl-1,4-oxazin-2-one

合成工艺路线路线简述

    阿克拉菌酮置于soybean Meal,Dipotassium Hydrogenphosphate,葡萄糖,Ke303 Of S. Galilaeus Ma144-M1,Magnesium Sulfate,Copper(II) Sulfate,Iron(II) Sulfate,Zinc(II) Sulfate,Sodium Chloride,Manganese(Ll) Chloride,Starch,Yeast Extract体系中,用 水 作为反应溶剂,化学反应 96.0H,反应生成 阿克拉霉素,Aclacinomycin X
    参考文献:New Betaclamycin And Aclarubicin Analogs Obtained By Prolonged Microbial Conversion With An Aclarubicin-Negative Mutant.
    标题:New Betaclamycin And Aclarubicin Analogs Obtained By Prolonged Microbial Conversion With An Aclarubicin-Negative Mutant.
    摘要:使用一种阿克拉霉素阴性链霉菌(streptomyces Galilaeus)突变体对β-罗多霉素酮和阿克拉维酮进行微生物转化,获得了新的蒽环类抗生素cg21-C和cg1-C,它们在每个加合的糖苷的c-7处具有红苷-2-脱氧岩藻糖基-罗多霉素三糖残基.它们仅在长时间转化培养时产生.由于通常的转化产物含有红苷-2-脱氧岩藻糖基-罗多霉素残基,在进一步培养过程中首先积累然后减少,很明显它们是通过末端红苷的修饰而产生的.本文描述了分离,纯化和结构测定,并讨论了体外对培养的l1210细胞的细胞毒性和形成机制.
    DOI:10.7164/antibiotics.49.669

    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-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-2010137421-A1
    优先权日:2006-11-08
    标题 :Small molecule therapeutics, synthesis of analogues and derivatives and methods of use
    发明人:THEODORAKIS EMMANUEL; BATOVA AYSE
    权利人:THEODORAKIS EMMANUEL; BATOVA AYSE
    摘要:Provided herein are compounds that are inducers of apoptosis activators of caspases and pharmaceutically acceptable derivatives thereof. Also provided are methods of synthesis of the compounds and methods for treatment of diseases in which there is uncontrolled cell growth and spread of abnormal cells, such as cancers, by administering the compounds.

    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:EP-0113566-A1
    优先权日:1982-12-20
    标题:New intermediate compounds for synthesis of aklavinones and their preparation
    发明人:KISHI YOSHITO
    权利人:MEIJI SEIKA KAISHA
    摘要:A new compound of the formulan wherein R, is a hydrogen atom, a hydroxyl group or an alkoxyl group of 1-4 carbon atoms and R 2 is an alkyl group of 1-4 carbon atoms is now provided. This new compound is useful as intermediate for synthesis of aklavinones which may be coupled with sugars, for example, daunosamine to give anthracycline antibiotics. The new compound of this invention is produced by several reaction steps started from a 3-halo-5-substituted or unsubstituted naphthoquinone and a furan diene compound. This process involves new regiospecific Diels-Alder condensation and new asymmetric crossed aldol condensation.

    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.
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    合成参考文献


    摘要:Japanese Journal of Antibiotics., 33(138), 1980 []
    摘要:Antibiotiki i Meditsinskaya Biotekhnologiya. Antibiotics and Medical Biotechnology., 30(918), 1985 []
    参考文献:10.1002/ijc.1419
    摘要:Kiguchi T, Niiya K, Shibakura M, Miyazono T, Shinagawa K, Ishimaru F, Kiura K, Ikeda K, Nakata Y, Harada M. Induction of urokinase-type plasminogen activator by the anthracycline antibiotic in human RC-K8 lymphoma and H69 lung-carcinoma cells. Int J Cancer. 2001 Sep;93(6):792–7. doi: 10.1002/ijc.1419.
    摘要:Kashima Y, Miyazaki M, Kaiho T, Ambiru S, Togawa A, Ohtsuka M, Sasada K, Shiobara M, Shimizu Y, Yoshioka S, Yoshidome H, Omoto H, Katoh A, Nakamura S, Nakajima N. A successful treatment for hepatocellular carcinoma with atrial tumor thrombus. Hepatogastroenterology. 1996 Jul;43(10):1041–5.
    参考文献:10.1023/a:1003549500211
    摘要:Juarranz A, Villanueva A, Cañete M, Polo S, Domínguez V, Stockert JC. Microscopical and Spectroscopic Studies on the Fluorescence of a Daunomycin–aluminum Complex. Journal of Molecular Histology. 1999 Mar;31(3):201–8. doi: 10.1023/a:1003549500211.
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