CAS: 254964-60-8; 4-Hydroxy-5-Methoxy-N,1-Dimethyl-2-Oxo-N-(4-(Trifluoromethyl)Phenyl)-1,2-Dihydroquinoline-3-Carboxamide
该化合物是一个小分子,其化学配方为C16H15N3O2, 主要是因其潜在的治疗应用而得到承认,特别是在肿瘤学方面;它是一种免疫分子,影响免疫系统对癌症的反应;Tasquinimod已知通过调节肿瘤微环境和加强抗肿瘤免疫,抑制肿瘤生长和转移;它的行动机制包括抑制血管产生和改变免疫细胞活动,特别是影响近类血源抑制细胞细胞细胞;该化合物一般是口服的,在包括前列腺癌在内的各种癌症临床试验中受到调查;Tasquinimod的安全情况和药理基因学一直是研究的课题,有助于对它进行评估,作为一种潜在的治疗选择.同许多研究药物一样,正在进行的研究旨在更好地了解其功效,最佳剂量和癌症治疗的长期影响.
- 英文名称4-Hydroxy-5-Methoxy-N,1-Dimethyl-2-Oxo-N-(4-(Trifluoromethyl)Phenyl)-1,2-Dihydroquinoline-3-Carboxamide
- 中文名称他喹莫德
- IUPAC名称4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-(4-(trifluoromethyl)phenyl)-1,2-dihydroquinoline-3-carboxamide
- 其它别名N-Methyl-N-(4-Trifluoromethyl-Phenyl)-1,2-Dihydro-4-Hydroxy-5-Methoxy-1-Methyl-2-Oxo-Quinoline-3-Carboxamide; 4-Hydroxy-5-Methoxy-N,1-Dimethyl-2-Oxo-N-[4-(Trifluoromethyl)Phenyl]Quinoline-3-Carboxamide; 4-Hydroxy-5-Methoxy-N
- CAS编号254964-60-8
- MFCD编号:MFCD18251454
- FDA UNII编号:756U07KN1R
- 分子式:C20H17F3N2O4分子量:406.36
- 产品CID: 1215886
- 产品分类生物化工 → 抑制剂 → 表观遗传学(Epigenetics)
物理性质
- 沸点501.5±50.0 °C at 760 mmHg
- 闪点257.1±30.1 °C
- 密度1.4±0.1 g/cm3
- pKa:4.50±1.00(预测)
- PSA:71.77
- LogP:2.63
- 折射率1.606
- 蒸汽压0.0±1.4 mmHg at 25°C
- 溶解性Insoluble In H2O; ≥20.32 mg/mL In DMSO; ≥4.75 mg/mL In Etoh With Gentle Warming And Ultrasonic
- 外观形态白色至淡黄色固体
- 储存条件2-8°C
- 产品应用该化合物是一种口服活性抗血管诱因剂,它通过对HDAC4信号的通氧抑制作用;它抑制通过同声抑制HDA4/N-COR/HDDA3依赖的HIF-1Α脱氧而产生肿瘤血管;它也以渗入流体细胞为目标,并通过阻止S100A9及其离子受体(RAGE和托氏感应器4)之间的相互作用来调节地方肿瘤免疫;在带有人类和鼠籍前列腺癌的老鼠模型中,TASKINIMOD(30毫克/千克/天,P.O.)显示出抗血管效应,从而抑制肿瘤生长.
MSDS等安全信息
上下游产品
CAS号22864-65-9 4-三氟甲基-N-甲基苯胺 | CAS号248282-18-0 4-羟基-5-甲氧基-1-甲基... | CAS号1354639-61-4 4-羟基-5-甲氧基-1-甲基... | CAS号248282-13-5 4-羟基-5-甲氧基-1-甲基... | CAS号53600-33-2 2-氨基-6-甲氧基苯甲酸 | CAS号67765-42-8 5-甲氧基-1H-苯并[d][... | CAS号91105-97-4 5-甲氧基-1-甲基-1H-苯...合成工艺路线路线简述
- 合成目标产物 Tasquinimod 主要起始原料 Methyl 4-Hydroxy-5-Methoxy-1-Methyl-2-Oxo-1,2-Dihydroquinoline-3-Carboxylate And 4-Trifluoromethyl-N-Methylaniline 97
- (文献来源)合成步骤主要原料 Methyl 4-Hydroxy-5-Methoxy-1-Methyl-2-Oxo-1,2-Dihydroquinoline-3-Carboxylate 和 4-Trifluoromethyl-N-Methylaniline 97
📜5-甲氧基-1-甲基-3,1-苯并恶嗪-2,4-二酮置于sodium Hydride体系中,用 N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 11.0H,反应生成他喹莫德
参考文献:Synthesis And Biological Evaluation Of New 1,2-Dihydro-4-Hydroxy-2-Oxo-3-Quinolinecarboxamides For Treatment Of Autoimmune Disorders: Structure−activity Relationship
标题:Synthesis And Biological Evaluation Of New 1,2-Dihydro-4-Hydroxy-2-Oxo-3-Quinolinecarboxamides For Treatment Of Autoimmune Disorders: Structure−activity Relationship
摘要:Roquinimex-Related 3-Quinolinecarboxamide Derivatives Were Prepared And Evaluated For Treatment Of Autoimmune Disorders. The Compounds Were Tested In Mice For Their Inhibitory Effects On Disease Development In The Acute Experimental Autoimmune Encephalomyelitis Model And Selected Compounds In The Beagle Dog For Induction Of Proinflammatory Reaction. Structure-Activity Relationships Are Discussed. Compound 8C,Laquinimod,Showed Improved Potency And Superior Toxicological Profile Compared To The Lead Compound Roquinimex (1B,Linomide) And Was Selected For Clinical Studies (Currently In Phase Ii).
Doi:10.1021/jm031044W
海关参考信息
- 2902300000-甲苯
2905110000-甲醇
2912110000-甲醛
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。
- 详情请参考：📖 海关编码查询和海关进出口税则
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: Li Z, Wu YH, Guo YQ, Min XJ, Lin Y. Tasquinimod promotes the sensitivity of ovarian cancer cells to cisplatin by down-regulating the HDAC4/p21 pathway. Korean J Physiol Pharmacol. 2024 Nov 14. doi: 10.4196/kjpp.24.132. Epub ahead of print.
36:317-329. doi: 10.1016/j.bioactmat.2024.03.004.
3: Wu S, Wang Y, Duan J, Teng Y, Wang D, Qi F. Identification of a shared gene signature and biological mechanism between diabetic foot ulcers and cutaneous lupus erythemnatosus by transcriptomic analysis. Front Physiol. 2024 Feb 16;15:1297810. doi: 10.3389/fphys.2024.1297810.
合成参考文献
参考文献:10.1007/s10637-011-9716-3
摘要:Rodrigues JR, Charris J, Ferrer R, Gamboa N, Angel J, Nitzsche B, Hoepfner M, Lein M, Jung K, Abramjuk C. Effect of quinolinyl acrylate derivatives on prostate cancer in vitro and in vivo. Invest New Drugs. 2012 Aug;30(4):1426–33. doi: 10.1007/s10637-011-9716-3.
参考文献:10.1002/pros.21435
摘要:George D, Moul JW. Emerging treatment options for patients with castration-resistant prostate cancer. Prostate. 2012 Feb;72(3):338–49. doi: 10.1002/pros.21435.
📝 需求与反馈
尽可能描述清楚需求与问题信息
