CAS: 1092351-67-1; 2-(4-Amino-1-Isopropyl-1H-Pyrazolo[3,4-D]Pyrimidin-3-yl)-1H-Indol-5-Ol
该化合物是一个小分子,主要作为某些动脉的选择性抑制器,特别是那些参与与癌症细胞扩散和生存有关的信号路径的分子,其特点是能够干扰特定酶的活动,从而调节细胞过程,如生长,分化和吸附等.托尔基尼b在肿瘤学中的潜在治疗应用,特别是在治疗表现出异常动脉活动的各类肿瘤方面的潜在治疗应用.该化合物的化学结构通常包括功能组,这些功能组增强了其与目标蛋白质的结合性,有助于其作为抑制剂的功效.此外,其药用皮质特性,例如吸收,分布,代谢和排泄物,对于确定其是否适合临床使用至关重要.与许多有针对性的疗法一样,正在进行的研究旨在阐明其生物效应和潜在副作用的全面范围,确保全面了解其在癌症治疗中的作用.
- 英文名称2-(4-Amino-1-Isopropyl-1H-Pyrazolo[3,4-D]Pyrimidin-3-yl)-1H-Indol-5-Ol
- 中文名称2-(4-氨基-1-异丙基-1H-吡唑并[3,4-D]嘧啶-3-基)-1H-吲哚-5-醇
- IUPAC名称2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
- 其它别名1H-Indol-5-Ol, 2-(4-Amino-1-(1-Methylethyl)-1H-Pyrazolo(3,4-D)Pyrimidin-3-yl)-; O,N-Dimethylhydroxyl-Amine Hydrochloride; 2-[4-Amino-1-(Propan-2-yl)-1H-Pyrazolo[3,4-D]Pyrimidin-3-Yl]-1H-Indol-5-Ol
- CAS编号1092351-67-1
- MFCD编号:MFCD12196869
- EINECS号:0
- FDA UNII编号:H5669VNZ7V
- 分子式:C16H16N6O分子量:308.35
- 产品CID: 127898
- 产品分类生物化工 → 抑制剂 → PI3K/Akt/mTOR抑制剂(PI3K/Akt/mTOR)
物理性质
- 熔点>187°C (分解)
- 沸点642.0±50.0 °C at 760 mmHg
- 闪点342.1±30.1 °C
- 密度1.6±0.1 g/cm3
- pKa:9.51±0.40(预测)
- PSA:105.64
- LogP:1.83
- 折射率1.800
- 蒸汽压0.0±2.0 mmHg at 25°C
- 溶解性DMSO(微溶),甲醇(微溶,超声处理)
- 外观形态固体-粉末
- 储存条件室温，干燥环境，密封保存
- 产品应用该化合物用作:抑制MTORC1和MTERC2复合体;诱发微发性硬化和吸附性;以依赖剂量的方式抑制AKT,P70S6K和S6的磷酸化;比对食肉素更有效地抑制依赖顶部的翻译;阻止各种癌症细胞线的扩散,包括白血病(例如SUP-B15,K562,P190-变换鼠标BM),多眼瘤(例如8226)和固态肿瘤细胞(例如,SKOV3,PC3,786-O,U87);推迟白血症的发作,促进老鼠模型中的白血糖回归;以及抑制雄性肿瘤的生长.
上下游产品
1-Isopropyl-3-(5-Methoxy-1H-Indol-2-yl)-1H-Pyrazolo[3,4-D]Pyrimidin-4-Amine 1203844-07-8合成工艺路线路线简述
📜3-碘-4-氨基吡唑并[3,4-D]嘧啶置于盐酸,四(三苯基膦)钯,Sodium Carbonate,Potassium Carbonate体系中,用 1,4-二氧六环,乙二醇二甲醚,水,N,N-二甲基甲酰胺 用作溶剂,化学反应生成2-(4-氨基-1-异丙基-1H-吡唑并[3,4-D]嘧啶-3-基)-1H-吲哚-5-醇
参考文献:Mtor Modulators And Uses Thereof
标题:Mtor Modulators And Uses Thereof
摘要:本发明提供了选择性调节特定蛋白激酶,尤其是mtor复合物的方法和组合物.该方法和组合物特别适用于选择性抑制mtor以用于治疗应用.
海关参考信息
- 2908199090-其他酚的卤化衍生物
2908999090-其他酚的硝化衍生物
2918290000-其他含酚基羧酸
2905199090-其他饱和一元醇 - 💡 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-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:US-2021220331-A1
优先权日:2016-05-03
标题:Inhibitors of ires-mediated protein synthesis
发明人：GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA
权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound
专利号:US-2024208898-A1
优先权日:2021-03-25
标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
发明人：KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
权利人:DANA FARBER CANCER INST INC
摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.
专利号:US-11299491-B2
优先权日:2018-11-16
标 题:Synthesis of key intermediate of KRAS G12C inhibitor compound
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Machova Urdzikova L, Cimermanova V, Karova K, Dominguez J, Stepankova K, Petrovicova M, Havelikova K, D Gandhi C, Jhanwar-Uniyal M, Jendelova P. The Role of Green Tea Catechin Epigallocatechin Gallate (EGCG) and Mammalian Target of Rapamycin (mTOR) Inhibitor PP242 (Torkinib) in the Treatment of Spinal Cord Injury. Antioxidants (Basel). 2023 Feb 3;12(2):363. doi: 10.3390/antiox12020363.
2: Koo J, Yue P, Deng X, Khuri FR, Sun SY. mTOR Complex 2 Stabilizes Mcl-1 Protein by Suppressing Its Glycogen Synthase Kinase 3-Dependent and SCF- FBXW7-Mediated Degradation. Mol Cell Biol. 2015 Jul;35(13):2344-55. doi: 10.1128/MCB.01525-14. Epub 2015 Apr 27.
3: Zhou K, Chen X, Zhang L, Yang Z, Zhu H, Guo D, Su R, Chen H, Li H, Song P, Xu X, Wang H, Zheng S, Xie H. Targeting peripheral immune organs with self- assembling prodrug nanoparticles ameliorates allogeneic heart transplant rejection. Am J Transplant. 2021 Dec;21(12):3871-3882. doi: 10.1111/ajt.16748. Epub 2021 Jul 19. 14(3):282. doi: 10.3390/ph14030282.
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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