CAS: 1300031-49-5; 7-(3,5-Dimethylisoxazol-4-yl)-8-Methoxy-1-((R)-1-(Pyridin-2-yl)Ethyl)-1H-Imidazo[4,5-C]Quinolin-2(3H)-One
该化合物是一个小分子抑制器,主要以其在针对蛋白的溴底和外缘家族(BET)的作用而闻名,该分子家族参与基因表达调节,该化合物在癌症研究领域引起了人们的注意,因为它有可能破坏蛋白质和直ones上的乙酰淋巴之间的相互作用,从而影响笔录调节.I-BET151的特点是它能够有选择地抑制蛋白,特别是BRD4, 它在各种癌症的蔓延中起着关键作用.该化合物通常被研究其对细胞扩散和差异的影响,以及其在血候恶性肿瘤和固态肿瘤中的潜在治疗应用.就物理特性而言,I-BET151在室温上是固态的,经常用于生物化学实验,以评价其功效和行动机制.其发展标志着有针对性的癌症疗法取得了显著进步,突出了对遗传基因的调节的重要性.
- 英文名称7-(3,5-Dimethylisoxazol-4-yl)-8-Methoxy-1-((R)-1-(Pyridin-2-yl)Ethyl)-1H-Imidazo[4,5-C]Quinolin-2(3H)-One
- 中文名称7-(3,5-二甲基异噁唑-4-基)-8-甲氧基-1-((R)-1-(吡啶-2-基)乙基)-1H-咪唑并[4,5-c]喹啉-2(3H)-酮
- IUPAC名称(R)-7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-(1-(pyridin-2-yl)ethyl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one
- 其它别名7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one
- CAS编号1300031-49-5
- MFCD编号:MFCD22124472
- EINECS号:802-803-9
- 分子式:C23H21N5O3
- 分子量:415.45
- 产品CID: 458692
- 产品分类生物化工 → 抑制剂 → 表观遗传学(Epigenetics)
物理性质
MSDS等安全信息
欧盟法规
C&L通报上下游产品
CAS号16114-47-9 3,5-二甲基异唑-4-硼酸 | CAS号5399-03-1 2-碘-4-硝基苯甲醚 | CAS号1300031-62-2 3,5-dimethyl-4-...合成工艺路线路线简述
- 合成目标产物 I-Bet151 (Gsk1210151A) 主要起始原料 3-Quinolinecarboxamide, 7-(3,5-Dimethyl-4-Isoxazolyl)-6-Methoxy-4-[[(1R)-1-(2-Pyridinyl)Ethyl]Amino]-
- (文献来源)合成步骤主要原料 3-Quinolinecarboxamide, 7-(3,5-Dimethyl-4-Isoxazolyl)-6-Methoxy-4-[[(1R)-1-(2-Pyridinyl)Ethyl]Amino]-
(R)-1-(2-吡啶)乙胺置于碘苯二乙酸,N,N-二异丙基乙胺,Potassium Hydroxide体系中,用 N-甲基吡咯烷酮,甲醇 用作溶剂,化学反应生成7-(3,5-二甲基异噁唑-4-基)-8-甲氧基-1-((R)-1-(吡啶-2-基)乙基)-1H-咪唑并[4,5-C]喹啉-2(3H)-酮
参考文献: Imidazo [4,5-C] Quinoline Derivates As Bromodomain Inhibitors[fr] Derives D'Imidazo [4,5-C] Quinoline Comme Inhibiteurs De Bromodomaine
标题: Imidazo [4,5-C] Quinoline Derivates As Bromodomain Inhibitors[fr] Derives D'Imidazo [4,5-C] Quinoline Comme Inhibiteurs De Bromodomaine
摘要:化合物的新颖结构式(i)及其盐,含有这种化合物的药物组合物以及它们在治疗中的应用.
海关参考信息
- 2905110000-甲醇
2933310010-吡啶
2908199090-其他酚的卤化衍生物
2908999090-其他酚的硝化衍生物 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
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.
专利号:CN-118754894-A
优先权日:2024-07-26
标题 :JQ1 derivative containing o-naphthoquinone structure, synthesis method thereof and application of JQ1 derivative in preparation of anti-triple-negative breast cancer drugs
专利号:CN-118812557-A
优先权日:2024-07-26
标 题:BRD4/GPX4 double-target inhibitor, synthesis method thereof and application of inhibitor in preparation of triple-negative breast cancer therapeutic drug
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📌 第三方产品分析报告
主要参考文献
1: Halper-Stromberg A, Lu CL, Klein F, Horwitz JA, Bournazos S, Nogueira L, Eisenreich TR, Liu C, Gazumyan A, Schaefer U, Furze RC, Seaman MS, Prinjha R, Tarakhovsky A, Ravetch JV, Nussenzweig MC. Broadly neutralizing antibodies and viral inducers decrease rebound from HIV-1 latent reservoirs in humanized mice. Cell. 2014 Aug 28;158(5):989-99. doi: 10.1016/j.cell.2014.07.043. Epub 2014 Aug 14.
2: Barrett E, Brothers S, Wahlestedt C, Beurel E. I-BET151 selectively regulates IL-6 production. Biochim Biophys Acta. 2014 Sep;1842(9):1549-55. doi: 10.1016/j.bbadis.2014.05.013. Epub 2014 May 22.
3: Pastori C, Daniel M, Penas C, Volmar CH, Johnstone AL, Brothers SP, Graham RM, Allen B, Sarkaria JN, Komotar RJ, Wahlestedt C, Ayad NG. BET bromodomain proteins are required for glioblastoma cell proliferation. Epigenetics. 2014 Apr;9(4):611-20. doi: 10.4161/epi.27906. Epub 2014 Feb 19.
合成参考文献
参考文献:10.4161/cc.23309
摘要:Boehm D, Calvanese V, Dar RD, Xing S, Schroeder S, Martins L, Aull K, Li PC, Planelles V, Bradner JE, Zhou MM, Siliciano RF, Weinberger L, Verdin E, Ott M. BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism. Cell Cycle. 2013 Feb 01;12(3):452–62.
参考文献:10.1016/j.bbadis.2014.05.013
摘要:Barrett E, Brothers S, Wahlestedt C, Beurel E. I-BET151 selectively regulates IL-6 production. Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease. 2014 Sep;1842(9):1549–55. doi: 10.1016/j.bbadis.2014.05.013.
参考文献:10.1021/acs.jmedchem.0c00566
摘要:Wellaway CR, Bamborough P, Bernard SG, Chung CW, Craggs PD, Cutler L, Demont EH, Evans JP, Gordon L, Karamshi B, Lewis AJ, Lindon MJ, Mitchell DJ, Rioja I, Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspiańska BS, Kerr WJ, Prinjha RK. Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype. J Med Chem. 2020 Sep 10;63(17):9020–44. doi: 10.1021/acs.jmedchem.0c00566.
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