CAS: 445430-58-0; N1-(1,8-Dimethylimidazo[1,2-A]Quinoxalin-4-yl)Ethane-1,2-Diamine
该化合物是IBKKT(IKK)的选择性强效抑制剂,具体针对IC50 的IC50 和 ~0.3 微米的IC50 亚单位.它显示对IKKTA和其他直流的高度选择性,使其成为研究NF-B信号路径的宝贵工具.BMS-3455441显示在减少细胞模型中的炎症和细胞皮生产方面的效力,支持在以炎症,免疫调节和癌症为重点的研究中使用.它的细胞渗透性性质允许在体外和外体内应用.该化合物具有良好的特性,具有可靠的批量和批量的一致性,确保机械学和药理学研究能够产生可复制的结果.
- 英文名称N1-(1,8-Dimethylimidazo[1,2-A]Quinoxalin-4-yl)Ethane-1,2-Diamine
- 中文名称N1-(1,8-二甲基咪唑并[1,2-a]喹噁啉-4-基)-1,2-乙二胺
- IUPAC名称N1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
- CAS编号445430-58-0
- MFCD编号:MFCD18089812
- FDA UNII编号:26SU0NEF5F
- 分子式:C14H17N5分子量:255.32
- 产品CID: 1453588
- 同类组份化合物CAS445430-58-0 (free base)547757-23-3 (HCl)445430-59-1 (2HCl)2320261-79-6 (TFA)
- 产品分类生物化工 → 抑制剂 → 核转录因子(NF→κB)
物理性质
- 沸点449.5±45.0 °C at 760 mmHg
- 闪点225.6±28.7 °C
- 密度1.3±0.1 g/cm3
- pKa:9.02±0.10(预测)
- PSA:68.24
- LogP:2.08
- 折射率1.696
- 蒸汽压0.0±1.1 mmHg at 25°C
- 溶解性Insoluble In H2O; ≥70 mg/mL In DMSO; ≥2.49 mg/mL In Etoh With Gentle Warming And Ultrasonic
- 外观形态白色至类白色粉末
- 储存条件在惰性气体(氮气或氩气)下 2–8 °C
- 产品应用该化合物用作IKK-2和IKK-1高选择性止热抑制剂,显示抗炎活动;抑制NF-XB信号并抑制生产亲食性细胞细胞炎(如TNF-Α,IL-1Β,IL-6,IAL-8);通过诱导细胞循环停用和吸附,显示血压和T细胞急性淋巴性白血病(T-ALL)模型的抗脉冲效应;改善微粒模型中的实验性热炎和凝固性诱发的炎;抑制TNVAL在内耳细胞中的粘合分子(ICAM-1和VCAM-1)的表达.
上下游产品
4-chloro-1,8-dimethylimidazo(1,2-a) quinoxaline ethylenediamineBMS-345541合成工艺路线路线简述
📜4-氯-1,8-二甲基咪唑[1,2-A]喹喔啉 以 甲醇,氯仿,乙二胺 作为反应溶剂,化学反应生成 N1-(1,8-二甲基咪唑并[1,2-A]喹噁啉-4-基)-1,2-乙二胺,3-碘萘-2-羧酸甲酯
参考文献:Methods Of Treating Inflammatory And Immune Diseases Using Inhibitors Of IKb Kinase (Ikk)
标题:Methods Of Treating Inflammatory And Immune Diseases Using Inhibitors Of IKb Kinase (Ikk)
摘要:本发明描述了利用iKb激酶(ikk)抑制剂预防和治疗炎症和免疫相关疾病或紊乱的方法.还描述了在体内证明有效用于预防和治疗炎症和免疫相关疾病或紊乱的ikk抑制剂.本发明的进一步实施方式涉及特定的ikk抑制剂,如4(2'-氨乙基)氨基-1,8-二甲基咪唑并[1,2-A]喹喔啉和化合物的结构式(I),其盐和药物组合物.
海关参考信息
- 2902300000-甲苯
2921211000-乙二胺 - 💡 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: Berger A, Quast SA, Plötz M, Kammermeier A, Eberle J. Sensitization of melanoma cells for TRAIL-induced apoptosis by BMS-345541 correlates with altered phosphorylation and activation of Bax. Cell Death Dis. 2013 Jan 24;4:e477. doi: 10.1038/cddis.2012.198.
2: Wu L, Shao L, Li M, Zheng J, Wang J, Feng W, Chang J, Wang Y, Hauer-Jensen M, Zhou D. BMS-345541 sensitizes MCF-7 breast cancer cells to ionizing radiation by selective inhibition of homologous recombinational repair of DNA double-strand breaks. Radiat Res. 2013 Feb;179(2):160-70. doi: 10.1667/RR3034.1. Epub 2012 Dec 21.
3: Buontempo F, Chiarini F, Bressanin D, Tabellini G, Melchionda F, Pession A, Fini M, Neri LM, McCubrey JA, Martelli AM. Activity of the selective IκB kinase inhibitor BMS-345541 against T-cell acute lymphoblastic leukemia: involvement of FOXO3a. Cell Cycle. 2012 Jul 1;11(13):2467-75. doi: 10.4161/cc.20859. Epub 2012 Jul 1. doi: 10.1089/jir.2012.0002. Epub 2012 Apr 17.
合成参考文献
参考文献:10.1016/j.jri.2009.09.005
摘要:Ito M, Nakashima A, Hidaka T, Okabe M, Bac ND, Ina S, Yoneda S, Shiozaki A, Sumi S, Tsuneyama K, Nikaido T, Saito S. A role for IL-17 in induction of an inflammation at the fetomaternal interface in preterm labour. Journal of Reproductive Immunology. 2010 Jan;84(1):75–85. doi: 10.1016/j.jri.2009.09.005.
参考文献:10.1667/rr3034.1
摘要:Wu L, Shao L, Li M, Zheng J, Wang J, Feng W, Chang J, Wang Y, Hauer-Jensen M, Zhou D. BMS-345541 sensitizes MCF-7 breast cancer cells to ionizing radiation by selective inhibition of homologous recombinational repair of DNA double-strand breaks. Radiat Res. 2013 Feb;179(2):160–70.
参考文献:10.1139/bcb-2016-0011
摘要:Gajalakshmi P, Majumder S, Viebahn CS, Swaminathan A, Yeoh GC, Chatterjee S. Interleukin-6 secreted by bipotential murine oval liver stem cells induces apoptosis of activated hepatic stellate cells by activating NF-κB-inducible nitric oxide synthase signaling. Biochem Cell Biol. 2017 Apr;95(2):263–72. doi: 10.1139/bcb-2016-0011.
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