CAS: 288150-92-5; 1-(6,8-Difluoro-2-Methylquinolin-4-yl)-3-(4-(Dimethylamino)Phenyl)Urea

该化合物是合成有机化合物,其结构复杂,包括松碱碱和尿素功能组.该化合物通常具有与quinoline和尿素类别有关的特性,如潜在的生物活动和有机溶剂中的溶液.氟原子在其结构中的存在可能会增强脂性并影响其药用植物基因特性.经常研究其在药用化学中的潜在应用,特别是在针对特定生物路径的药品开发中.二甲基氨基化合物可能有助于其基本性和总体再活动.与许多合成化合物一样,安全性和处理预防措施必不可少,因为它们如果不得到适当管理,可能会带来风险.

结构式图片

物理性质

MSDS等安全信息

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-11285169-B2
    优先权日:2013-03-13
    标题 :Methods for modulating chemotherapeutic cytotoxicity
    发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
    权利人:US HEALTH
    摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

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    主要参考文献


    1: Langmead CJ, Jerman JC, Brough SJ, Scott C, Porter RA, Herdon HJ. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141(2):340-6. doi: 10.1038/sj.bjp.0705610. Epub 2003 Dec 22.
    2: Tissen I, Kurbanov R, Hohlov K, Proshin S, Lebedev A, Bagaturiya G, Shabanov P. OX1R ANTAGONIST SB408124 ACTION AND EXTRAHYPOTHALAMIC CRF IN RATS AFTER PSYCHOTRAUMATIC EXPOSURE. Georgian Med News. 2019 May;(290):127-131. 7(7):e39131. doi: 10.1371/journal.pone.0039131. Epub 2012 Jul 2.
    4: Valiante S, Liguori G, Tafuri S, Pavone LM, Campese R, Monaco R, Iachetta G, Assisi L, Mirabella N, Forte M, Costagliola A, Vittoria A. Expression and potential role of the peptide orexin-A in prostate cancer. Biochem Biophys Res Commun. 2015 Sep 4;464(4):1290-1296. doi: 10.1016/j.bbrc.2015.07.124. Epub 2015 Jul 26. 215(1):191-203. doi: 10.1007/s00213-010-2127-x. Epub 2010 Dec 22. 177(1-3):46-52. doi: 10.1016/j.regpep.2012.04.007. Epub 2012 May 2. 1864(11):3618-3628. doi: 10.1016/j.bbadis.2018.08.023. Epub 2018 Aug 18. 352(3):590-601. doi: 10.1124/jpet.114.220392. Epub 2015 Jan 12.

    合成参考文献


    参考文献:10.1016/j.neuroscience.2014.08.017
    摘要:Choudhary RC, Khanday MA, Mitra A, Mallick BN. Perifornical orexinergic neurons modulate REM sleep by influencing locus coeruleus neurons in rats. Neuroscience. 2014 Oct 24;279():33–43. doi: 10.1016/j.neuroscience.2014.08.017.
    参考文献:10.1007/s11906-018-0879-6
    摘要:Sieminski M, Szypenbejl J, Partinen E. Orexins, Sleep, and Blood Pressure. Current Hypertension Reports. 2018 Jul 10;20(9):79. doi: 10.1007/s11906-018-0879-6.
    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
    参考文献:10.1007/978-3-031-07897-2_10
    摘要:Fathima S, Murala S, Bollu PC. Orexins. 2022. In: Neurochemistry in Clinical Practice.
    参考文献:10.1124/jpet.114.220392
    摘要:Bonaventure P, Yun S, Johnson PL, Shekhar A, Fitz SD, Shireman BT, Lebold TP, Nepomuceno D, Lord B, Wennerholm M, Shelton J, Carruthers N, Lovenberg T, Dugovic C. A Selective Orexin-1 Receptor Antagonist Attenuates Stress-Induced Hyperarousal without Hypnotic Effects. The Journal of Pharmacology and Experimental Therapeutics. 2015 Mar;352(3):590–601. doi: 10.1124/jpet.114.220392.
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