CAS: 900185-01-5; 2-((4-Amino-1H-Pyrazolo[3,4-D]Pyrimidin-1-yl)Methyl)-5-Methyl-3-(O-Tolyl)Quinazolin-4(3H)-One

该化合物是它有能力有选择地抑制PIK-3K的具体形态,这可能导致细胞扩散减少,并增加某些癌症细胞线的吸附性;PIK-293通常在其药理效应,潜在副作用及其在混合疗法中的作用方面进行研究;其溶性,稳定性和生物利用率是影响其在生物系统中功效的重要因素;与许多实验性化合物一样, 正在进行的研究对于充分了解其行动机制,治疗潜力和临床应用安全性简介至关重要.

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上下游产品

o-toluidineo-toluidine 2-amino-6-methylbenzoic acid 2-(chloromethyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one pyrimidin4-Aminopyrazolo3,4-dpyrimidin

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    专利信息


    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    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

    Zhu, J., Li, K., Yu, L., Chen, Y., Cai, Y., Jin, J., & Hou, T. (2021). Targeting phosphatidylinositol 3‐kinase gamma (PI3Kγ): Discovery and development of its selective inhibitors. Medicinal research reviews, 41(3), 1599-1621. Cmiljanović, N. (2011). Development of novel, potent and selective small molecular weight PI3K/mTOR inhibitors for the treatment of cancer (Doctoral dissertation, University_of_Basel). Chandra Joshi, M., Kumar, K., & Kumar, V. (2014). Potent phosphatidylinositol 3-kinase inhibitors and their biology. Current drug discovery technologies, 11(2), 113-126.

    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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