CAS: 956905-27-4; 2-(4-(1-(Quinolin-6-Ylmethyl)-1H-[1,2,3]Triazolo[4,5-B]Pyrazin-6-yl)-1H-Pyrazol-1-yl)Ethan-1-Ol

该化合物是一种选择性的C-Met 动脉抑制器,在针对异常的HGF/c-Met信号信号路径的临床前研究中表现出效力.C-Met的高度特殊性可以将非目标效果降到最低,使其成为调查诱因机制和潜在治疗应用的宝贵工具.该复合物展示了防止C-Met磷酸化的强大抑制性活动,干扰了肿瘤扩散,入侵和转移的下游信号级. PF-04217903在研究环境中被用于探索C-Met依赖性恶性肿瘤和抗药机制.其精密的药性成形相色特征和选择性使得它适合体外和体外研究,对以细胞为动力的癌症生物学提供洞察,并支持定向疗法的发展.

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上下游产品

6-溴-1-(喹啉-6-甲基)-1H-1,2,3-噻唑并[4,5-B]吡嗪 6-((6-Bromo-1H-[1,2,3]Triazolo[4,5-B]Pyrazin-1-yl)-Methyl)Quinoline 956907-14-5

合成工艺路线路线简述

  • 956907-32-7 = 956905-27-4
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Dichloromethane,1,4-Dioxane; Rt; 1 H,Rt1.2 Reagents: Sodium Carbonate; Ph 7,Rt
    标题:Discovery Of A Novel Class Of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (C-Met) Protein Kinase Inhibitors And Identification Of The Clinical Candidate 2-(4-(1-(Quinolin-6-Ylmethyl)-1H-[1,2,3]Triazolo[4,5-B]Pyrazin-6-Yl)-1H-Pyrazol-1-Yl)Ethanol (Pf-04217903) For The Treatment Of Cancer
    作者:Cui,J. Jean; Mctigue,Michele; Nambu,Mitchell; Tran-Dube,Michelle; Pairish,Mason; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(18) 页码:8091-8109]

    = 956905-27-4 [标题:Reaction Conditions
    标题:Discovery Of A Novel Class Of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (C-Met) Protein Kinase Inhibitors And Identification Of The Clinical Candidate 2-(4-(1-(Quinolin-6-Ylmethyl)-1H-[1,2,3]Triazolo[4,5-B]Pyrazin-6-Yl)-1H-Pyrazol-1-Yl)Ethanol (Pf-04217903) For The Treatment Of Cancer [erratum To Document Cited In Ca157:492637]
    作者:Cui,J. Jean; Mctigue,Michele; Nambu,Mitchell; Tran-Dube,Michelle; Pairish,Mason; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(22)]

    = 956905-27-4 + 75-75-2 [标题:Reaction Conditions
    标题:Discovery Of A Novel Class Of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (C-Met) Protein Kinase Inhibitors And Identification Of The Clinical Candidate 2-(4-(1-(Quinolin-6-Ylmethyl)-1H-[1,2,3]Triazolo[4,5-B]Pyrazin-6-Yl)-1H-Pyrazol-1-Yl)Ethanol (Pf-04217903) For The Treatment Of Cancer [erratum To Document Cited In Ca157:492637]
    作者:Cui,J. Jean; Mctigue,Michele; Nambu,Mitchell; Tran-Dube,Michelle; Pairish,Mason; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(22)]

    = 956905-27-4 + 75-75-2 [标题:Reaction Conditions
    标题:Discovery Of A Novel Class Of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (C-Met) Protein Kinase Inhibitors And Identification Of The Clinical Candidate 2-(4-(1-(Quinolin-6-Ylmethyl)-1H-[1,2,3]Triazolo[4,5-B]Pyrazin-6-Yl)-1H-Pyrazol-1-Yl)Ethanol (Pf-04217903) For The Treatment Of Cancer
    作者:Cui,J. Jean; Mctigue,Michele; Nambu,Mitchell; Tran-Dube,Michelle; Pairish,Mason; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2012 卷标:55(18) 页码:8091-8109
📜6-氨基甲基喹啉置于盐酸,1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,异戊腈,Caesium Carbonate,N,N-二异丙基乙胺体系中,用 1,4-二氧六环,乙二醇二甲醚,二氯甲烷,水,N,N-二甲基甲酰胺,正丁醇 作为反应溶剂,化学反应 65.0H,反应生成 Pf 04217903; 2-[4-[1-(喹啉-6-甲基)-1H-[1,2,3]三唑并[4,5-B]吡嗪-6-基]-1H-吡唑-1-基]乙醇
参考文献:一类新型的选择性间质-上皮转换因子(c-Met)蛋白激酶抑制剂的发现及临床候选药物2-(4-(1-(quinolin-6-Ylmethyl)-1 H-[1,2]的鉴定,3]三唑并[4,5-B]吡嗪-6-基)-1 H-吡唑-1-基)乙醇(pf-04217903)用于治疗癌症
标题:一类新型的选择性间质-上皮转换因子(c-Met)蛋白激酶抑制剂的发现及临床候选药物2-(4-(1-(quinolin-6-Ylmethyl)-1 H-[1,2]的鉴定,3]三唑并[4,5-B]吡嗪-6-基)-1 H-吡唑-1-基)乙醇(pf-04217903)用于治疗癌症
摘要:C-Met受体酪氨酸激酶因其在人类肿瘤发生和肿瘤进展中的关键作用而成为有吸引力的肿瘤学靶标.在c-Met Hts运动期间发现了羟吲哚酰肼第6点,随后证明对多种其他激酶具有不同寻常的选择性.相关的羟吲哚酰肼c-Met抑制剂10与非磷酸化的c-Met激酶结构域的共晶体结构揭示了与精美的选择性谱相关的独特结合模式.使用基于结构的药物设计,将化学不稳定的羟吲哚酰肼支架替换为化学和代谢稳定的三唑并吡嗪支架.药物化学先导物优化产生的2-(4-(1-(喹啉-6-基甲基)-1 ħ-[1,2,3]三唑并[4,5-B]吡嗪-6-基)-1 H-吡唑-1-基)乙醇(2,Pf-04217903),一种非常有效且选择性极强的c-Met抑制剂.图2证明了在c-Met依赖性肿瘤模型中具有非常好的口服pk特性和在临床前研究中可接受的安全性,有效地抑制了肿瘤生长.2进入了i期肿瘤学环境的临床评估.
DOI:10.1021/jm300967G

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专利信息


专利号:WO-2025128098-A1
优先权日:2023-12-13
标 题 :Solid oral dosage forms, kits, and methods of using the same
发明人：LI YING; LANGER ROBERT; TRAVERSO CARLO
权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

专利号:US-12180228-B2
优先权日:2019-06-05
标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
发明人：MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

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主要参考文献


1: Zhou W, Lin L, Chen D, Wang J, Chen J. Construction of a Liver Cancer Prognostic Model Based on Interferon-Gamma-Related Genes for Revealing the Immune Landscape. J Environ Pathol Toxicol Oncol. 2024;43(4):25-42. doi: 10.1615/JEnvironPatholToxicolOncol.2024049848.
2023:8347759. doi: 10.1155/2023/8347759.
3: Felix FB, Dias J, Vago JP, Martins DG, Beltrami VA, Fernandes DO, Menezes Dos Santos ACP, Queiroz-Junior CM, de Sousa LP, Amaral FA, Soriani FM, Teixeira MM, Pinho V. Blocking the HGF-MET pathway induces resolution of neutrophilic inflammation by promoting neutrophil apoptosis and efferocytosis. Pharmacol Res. 2023 Feb;188:106640. doi: 10.1016/j.phrs.2022.106640. Epub 2023 Jan 7. 11(11):5127-5142. doi: 10.7150/thno.54741.

合成参考文献


参考文献:10.1186/s13046-018-0750-2
摘要:Zhang Y, Gao X, Zhu Y, Kadel D, Sun H, Chen J, Luo Q, Sun H, Yang L, Yang J, Sheng Y, Zheng Y, Zhu K, Dong Q, Qin L. The dual blockade of MET and VEGFR2 signaling demonstrates pronounced inhibition on tumor growth and metastasis of hepatocellular carcinoma. Journal of Experimental & Clinical Cancer Research. 2018 Apr 30;37(1):93. doi: 10.1186/s13046-018-0750-2.
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