CAS: 948557-43-5; 4-(4-(6-Methoxynaphthalen-2-yl)-2-(4-(Methylsulfinyl)Phenyl)-1H-Imidazol-5-yl)Pyridine
该化合物是针对铁氏2 (TEK) 受体抗体抗体强力的选择性小分子抑制器,在血管产生和血管稳定性方面起着关键作用.这种复合物具有很强的能性与特性,有效地抑制了铁氏2磷酸化和下游信号路径.其特征清晰的行动机制使它成为研究生理和病理环境中与血管产生有关的过程,例如癌症和血管畸形的一个宝贵工具.抑制器显示在体外有有利的生化活动,并被用于临床前研究,以阐明依靠铁氏2的细胞反应.其稳定性和选择性特征确保可靠的实验性再传播,支持其在机械和治疗性调查中的应用.
- 英文名称4-(4-(6-Methoxynaphthalen-2-yl)-2-(4-(Methylsulfinyl)Phenyl)-1H-Imidazol-5-yl)Pyridine
- 中文名称TIE2激酶抑制剂
- IUPAC名称4-(4-(6-methoxynaphthalen-2-yl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine
- 其它别名Tie2 In 5; Tie2In5; Tie2 Inhibitor 5; Tie2-Inhibitor-5; Tie2 Kinase Inhibitor 5; Tie2 Kinase-In-1; Tie2 Kinase Inhibitor 1; Tie2 Kinas
- CAS编号948557-43-5
- MFCD编号:MFCD18384977
- 分子式:C26H21N3O2S分子量:439.54
- 产品CID: 2001164
- 产品分类生物化工 → 抑制剂 → 蛋白酪氨酸激酶
物理性质
- 沸点699.8±55.0 °C at 760 mmHg
- 闪点377.0±31.5 °C
- 密度1.4±0.1 g/cm3
- pKa:9.53±0.10(预测)
- PSA:87.08
- LogP:5.31
- 折射率1.746
- 蒸汽压0.0±2.1 mmHg at 25°C
- 溶解性≥22 mg/mL In DMSO; Insoluble In H2O; Insoluble In Etoh
- 外观形态淡黄色至黄色粉末
- 储存条件2-8°C(避光保存)
- 产品应用该化合物是TIE2受体的选择性抑制剂,一种主要表现在内皮细胞上并参与血管发育和血管生成的受体性强氧素流动酶,其目标为TIE2:TIE2.IN-5调节器以铁皮血管稳定性和内皮纤维功能为目标,使其成为癌症和糖尿病复发等异常血管生成疾病的潜在治疗剂.关于TIE2/IN-5的研究探讨了其在调节血管形成,炎症和肿瘤生长方面的作用,并应用于癌症治疗和其他与血管生成有关的疾病.
合成工艺路线路线简述
- 427895-98-5 + 3446-89-7 = 948557-43-5
反应条件:1.1 Reagents: Ammonium Acetate Solvents: Acetic Acid; Reflux1.2 Reagents: Trimethyl Phosphite Solvents: Dimethylformamide; Reflux1.3 Reagents: Acetic Acid,Potassium Persulfate Solvents: Water
标题:Pyridinylimidazole Inhibitors Of Tie2 Kinase
作者:Semones,Marcus; Feng,Yanhong; Johnson,Neil; Adams,Jerry L.; Winkler,Jim; Et Al
参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2007 卷标:17(17) 页码:4756-4760]
427895-98-5 + 3446-89-7 = 948557-43-5
反应条件:1.1 Reagents: Ammonium Hydroxide Solvents: Acetic Acid; 90 °C1.2 Reagents: Trimethyl Phosphite Solvents: Dimethylformamide; 90 °C1.3 Reagents: Potassium Persulfate
标题:Optimization Of Triarylimidazoles For Tie2: Influence Of Conformation On Potency
作者:Johnson,Neil W.; Semones,Marcus; Adams,Jerry L.; Hansbury,Michael; Winkler,Jim
参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2007 卷标:17(20) 页码:5514-5517
📜在 Dipotassium Peroxodisulfate,溶剂黄146体系中,用 水 作为反应溶剂,化学反应生成 Tie2激酶抑制剂
参考文献:Pyridinylimidazole Inhibitors Of Tie2 Kinase
标题:Pyridinylimidazole Inhibitors Of Tie2 Kinase
摘要:This Communication Details The Evolution Of The Screening Lead Sb-203580,A Known Csbp/p38 Kinase Inhibitor,Into A Potent And Selective Tie2 Tyrosine Kinase Inhibitor. The Optimized Compound 5 Showed Efficacy In An In Vivo Model Of Angiogenesis And A Mopc-315 Plasmacytoma Xenograft Model. (C) 2007 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2007.06.068
海关参考信息
- 2902902000-精萘
2905110000-甲醇
2933310010-吡啶
2908199090-其他酚的卤化衍生物 - 💡 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:JP-2012512172-A
优先权日:2008-12-15
标 题:Stereoselective synthesis of piperidine derivatives.
专利号:TW-I386395-B
优先权日:2008-12-15
标 题:Stereoselective synthesis of piperidine derivatives
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: El-Damasy AK, Cho NC, Nam G, Pae AN, Keum G. Discovery of a Nanomolar Multikinase Inhibitor (KST016366): A New Benzothiazole Derivative with Remarkable Broad-Spectrum Antiproliferative Activity. ChemMedChem. 2016 Aug 5;11(15):1587-95. doi: 10.1002/cmdc.201600224. Epub 2016 Jul 12. doi: 10.1021/tx500518j. Epub 2015 Apr 21. Epub 2007 Jun 27.
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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