CAS: 1887069-10-4; (R)-3-((2-Chloro-5-(Ethoxymethyl)Pyrimidin-4-yl)Oxy)-10-Methyl-9,10,11,12-Tetrahydro-8H-[1,4]Diazepino[5',6':4,5]Thieno[3,2-F]Quinolin-8-One
该化合物是一种选择性的小型分子抑制剂,针对与诱导诱导信号有牵连的特定动脉路径,其行动机制涉及与变异体的动脉异形结合的高度亲近性,从而抑制畸形细胞扩散,在恶性细胞中促进流行性疾病.临床研究显示,它以有利的药用植物基因特征抑制肿瘤生长的效果,包括良好的口服生物利用率和持续的目标接触.Gamcemetinib 显示,与早代抑制器相比,目标外效应已经减少,加强了治疗窗口.其潜在应用包括治疗受目标动脉突变驱动的恶性肿瘤,特别是在抗药性或耐性病例中.正在进行进一步的临床评估,以验证其对人类试验的安全性和有效性.
- 英文名称(R)-3-((2-Chloro-5-(Ethoxymethyl)Pyrimidin-4-yl)Oxy)-10-Methyl-9,10,11,12-Tetrahydro-8H-[1,4]Diazepino[5',6':4,5]Thieno[3,2-F]Quinolin-8-One
- 中文名称(R)-3-((2-氯-5-(乙氧基甲基)嘧啶-4-基)氧基)-10-甲基-9,10,11,12-四氢-8H-[1,4]HO[5',6':4,5]噻吩并[3,2-F]喹啉-8-酮
- IUPAC名称(R)-3-((2-chloro-5-(ethoxymethyl)pyrimidin-4-yl)oxy)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
- 其它别名8H-[1,4]Diazepino[5',6':4,5]Thieno[3,2-F]Quinolin-8-One, 3-[[2-Chloro-5-(Ethoxymethyl)-4-Pyrimidinyl]Oxy]-9,10,11,12-Tetrahydro-10-Methyl-, (10R)-; Gamcemetinib; Gamcemetinib; (R)-3-((2-Chloro-5-(Ethoxymethyl)Pyrimidin-4-yl)Oxy)-10-Methyl-9,10,11,12-Tetrahydro-8H-[1,4]Diazepino[5',6':4,5]Thieno[3,2-F]Quinolin-8-One; (R)-3-((2-Chloro-5-(Ethoxymethyl)Pyrimidin-4-yl)Oxy)-10-Methyl-9,10,11,12-Tetrahydro-8H-[1,4]Diazepino[5',6':4,5]Thieno[3,2-F]Quinolin-8-One
- CAS编号1887069-10-4
- MFCD编号:MFCD34567774
- FDA UNII编号:OS2IR8TV1O
- 分子式:C22H20ClN5O3S分子量:469.95
- 产品CID: 956946
- 同类组份化合物CAS1887069-10-4
- 产品分类Inhibitors/Agonists → Cell Cycle → HSP
物理性质
MSDS等安全信息
合成工艺路线路线简述
海关参考信息
- 2902200000-苯
2912110000-甲醛
2921211000-乙二胺
2933310010-吡啶 - 💡 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。
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专利信息
专利号:US-11655257-B2
优先权日:2017-03-16
标 题:MK2 inhibitors, synthesis thereof, and intermediates thereto
发明人：FEIGELSON GREGG BRIAN; GEHERTY MARYLL E; HEID JR RICHARD MARTIN; KOTHARE MOHIT; MAN HON-WAH; RUCHELMAN ALEXANDER L; TRAVERSE JOHN F; YONG KELVIN HIN-YEONG; ZHANG CHENGMIN
权利人:CELGENE CAR LLC
摘要:The present invention provides methods of preparing a MK2 inhibitor, and intermediates related thereto.
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
Schwarz, M., Kurkunov, M., Wittlinger, F., Rudalska, R., Wang, G., Schwalm, M. P., ... & Gehringer, M. (2024). Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles. Journal of medicinal chemistry, 67(8), 6549-6569. Hillebrand, L., Liang, X. J., Serafim, R. A., & Gehringer, M. (2024). Emerging and re-emerging warheads for targeted covalent inhibitors: an update. Journal of medicinal chemistry, 67(10), 7668-7758. Schultz, C. R., Swanson, M. A., Dowling, T. C., & Bachmann, A. S. central maleimide Menu. Dahl, A. (2017). Rufinamide is an anticonvulsant medication Menu.合成参考文献
参考文献:10.1021/acs.jmedchem.3c02483
摘要:Schwarz M, Kurkunov M, Wittlinger F, Rudalska R, Wang G, Schwalm MP, Rasch A, Wagner B, Laufer SA, Knapp S, Dauch D, Gehringer M. Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles. J Med Chem. 2024 Apr 25;67(8):6549–69. doi: 10.1021/acs.jmedchem.3c02483.
参考文献:10.1021/acs.jmedchem.3c01825
摘要:Hillebrand L, Liang XJ, Serafim RAM, Gehringer M. Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update. J Med Chem. 2024 May 23;67(10):7668–758. doi: 10.1021/acs.jmedchem.3c01825.
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