CAS: 841290-81-1; 6-((5-Fluoro-2-((3,4,5-Trimethoxyphenyl)Amino)Pyrimidin-4-yl)Amino)-2,2-Dimethyl-2H-Pyrido[3,2-B][1,4]Oxazin-3(4H)-One Benzenesulfonate
- 英文名称6-((5-Fluoro-2-((3,4,5-Trimethoxyphenyl)Amino)Pyrimidin-4-yl)Amino)-2,2-Dimethyl-2H-Pyrido[3,2-B][1,4]Oxazin-3(4H)-One Benzenesulfonate
- 中文名称6-[[5-氟-2-[(3,4,5-三甲氧基苯基)氨基]-4-嘧啶基]氨基]-2,2-二甲基-2H-吡啶并[3,2-b]-1,4-恶嗪-3(4H)-酮苯磺酸盐
- IUPAC名称6-((5-fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one benzenesulfonate
- CAS编号841290-81-1
- MFCD编号:MFCD18385012
- 分子式:C28H29FN6O8S分子量:628.64
- 产品CID: 1829740
- 同类组份化合物CAS841290-81-1 (besylate)841290-80-0 (free base)
- 产品分类生物化工 → 抑制剂 → 血管生成(Angiogenesis)
物理性质
- PSA:198.22
- LogP:5.2273
- 溶解性≥31.45 mg/mL In DMSO; Insoluble In H2O; ≥14.95 mg/mL In Etoh With Ultrasonic
- 外观形态淡黄色至卡其色固体
- 储存条件储存在 -20°C
- 产品应用该化合物用作在慢性淋巴细胞细胞中诱发吸附性硬化症的强效SYK抑制剂;抑制单细胞/腺细胞和中微营养素中依赖SYKS的受体调节活动;B淋巴囊细胞中B-细胞受体(BCR)的阻隔信号;抑制IGE和IGG的受受体信号;阻止LTC4,细胞(如TNFΑ,IL-8)和MEST细胞中GM-CSF的生产和释放;有效减轻抗体诱发性节炎和皮肤反向被动阿瑟反应动物模型中的炎性反应;还调查其在以最小的免疫毒性治疗自燃性疾病和炎性疾病方面的潜力.
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海关参考信息
- 2905122000-异丙醇
2905143000-叔丁醇
2907210001-间苯二酚
2907221000-对苯二酚 - 💡 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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供应商参考报价(招募中)
品牌试剂参考报价(招募中)
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主要参考文献
1: Rolf MG, Curwen JO, Veldman-Jones M, Eberlein C, Wang J, Harmer A, Hellawell CJ, Braddock M. In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib. Pharmacol Res Perspect. 2015 Oct;3(5):e00175. doi: 10.1002/prp2.175. Epub 2015 Sep 4.
2: Borge M, Remes Lenicov F, Nannini PR, de los Ríos Alicandú MM, Podaza E, Ceballos A, Fernández Grecco H, Cabrejo M, Bezares RF, Morande PE, Oppezzo P, Giordano M, Gamberale R. The expression of sphingosine-1 phosphate receptor-1 in chronic lymphocytic leukemia cells is impaired by tumor microenvironmental signals and enhanced by piceatannol and R406. J Immunol. 2014 Sep 15;193(6):3165-74. doi: 10.4049/jimmunol.1400547. Epub 2014 Aug 15. doi: 10.1007/s11095-014-1399-y. Epub 2014 Jun 7.
4: Lhermusier T, van Rottem J, Garcia C, Xuereb JM, Ragab A, Martin V, Gratacap MP, Sié P, Payrastre B. The Syk-kinase inhibitor R406 impairs platelet activation and monocyte tissue factor expression triggered by heparin-PF4 complex directed antibodies. J Thromb Haemost. 2011 Oct;9(10):2067-76. doi: 10.1111/j.1538-7836.2011.04470.x. doi: 10.3109/00498251003734244. doi: 10.1124/dmd.110.032151. Epub 2010 Apr 6. doi: 10.1182/blood-2009-03-212837. Epub 2009 Jun 2. doi: 10.1111/j.1538-7836.2009.03451.x. Epub 2009 Apr 24. Epub 2007 Mar 31. Epub 2006 Aug 31. Erratum in: J Pharmacol Exp Ther. 2013 May;345(2):326.
合成参考文献
参考文献:10.1016/j.taap.2018.06.022
摘要:Lim H, Min DS, Park H, Kim HP. Flavonoids interfere with NLRP3 inflammasome activation. Toxicol Appl Pharmacol. 2018 Sep 15;355():93–102. doi: 10.1016/j.taap.2018.06.022.
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