CAS: 1062169-56-5; Methyl 4-(6-(4-((Methoxycarbonyl)Amino)Phenyl)-4-Morpholino-1H-Pyrazolo[3,4-D]Pyrimidin-1-yl)Piperidine-1-Carboxylate

该化合物是医学化学领域,特别是其潜在的治疗应用领域引起注意的一种化学化合物,被归类为小分子抑制剂,具体针对某些蛋白性血管,在包括细胞生长和分裂在内的各种细胞过程中发挥着关键作用;该化合物展示了一种独特的结构,使其能够有选择地与其目标互动,有可能导致与癌症等疾病有关的信号路径的调节;WYE-354, 已经就其在临床前模式中的效力进行了研究,显示出抑制肿瘤生长的有希望的结果;此外,其药用植物特性,如吸收,分布,代谢和排泄,对于确定是否适合作为治疗剂进一步发展至关重要;随着研究的继续,WYE-354可能有助于在肿瘤和其他相关领域推进有针对性的治疗;然而,为了充分了解其安全性特征和治疗潜力,必须进行详细研究.

结构式图片

上下游产品

methanol bis(trichloromethyl) carbonate methyl 4-[6-(4-aminophenyl)-4-morpholin-4-yl-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate

合成工艺路线路线简述

    📜甲醇,三光气,Methyl 4-[6-(4-Aminophenyl)-4-Morpholin-4-Yl-1H-Pyrazolo[3,4-D]Pyrimidin-1-Yl]Piperidine-1-Carboxylate置于三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 0.08H,以23%的收率获得wye 354; 4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-D]嘧啶-1-基]-1-哌啶羧酸甲酯
    参考文献:雷帕霉素哺乳动物靶标的atp竞争性抑制剂:高强度和选择性吡唑并嘧啶的设计和合成
    标题:雷帕霉素哺乳动物靶标的atp竞争性抑制剂:高强度和选择性吡唑并嘧啶的设计和合成
    摘要:雷帕霉素(mtor)的哺乳动物靶标是生长,存活和代谢的主要调节剂,是经过验证的癌症治疗靶标.雷帕霉素及其类似物(mtor的变构抑制剂)仅部分抑制一种mtor蛋白复合物.描述了具有增强抗癌功效潜力的atp竞争性mtor整体抑制剂.鉴定并完善了导致效价和选择性的结构特征,从而在肿瘤异种移植模型中产生了具有体内功效的化合物.
    Doi:10.1021/jm900851F

    专利信息


    专利号:CN-108379591-B
    优先权日:2018-04-03
    标 题 :Synthesis of Immune Agonist Targeting Compounds and Their Applications

    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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    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: Wahdan-Alaswad RS, Bane KL, Song K, Shola DT, Garcia JA, Danielpour D. Inhibition of mTORC1 kinase activates Smads 1 and 5 but not Smad8 in human prostate cancer cells, mediating cytostatic response to rapamycin. Mol Cancer Res. 2012 Jun;10(6):821-33. doi: 10.1158/1541-7786.MCR-11-0615. Epub 2012 Mar 27.

    合成参考文献


    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.
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