R406|841290-81-1|-陌孚医药/Medlife

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R406

目录号: PL11560 纯度: ≥98%

CAS No. :841290-81-1

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中文名称	R406
中文别名	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;R406(苯磺酸盐);R406（苯磺酸盐）抑制剂
英文名称	R406
英文别名	2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one,6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-, monobenzenesulfonate;R406 Benzenesulfonate;2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one,6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimid...;2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one,6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-, mono;benzenesulfonic acid,6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one;R 406;R406 tosilate;R-406;R406
Cas No.	841290-81-1
分子式	C₂₂H₂₃N₆O₅F^.C₆H₆O₃S
分子量	628.63
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	R406 是一种有效的，具有口服活性的，ATP竞争性的 Syk/FLT3 抑制剂，K_i 为 30 nM，有效抑制 Syk 激酶活性，IC₅₀ 为 41 nM。R406 可减轻免疫复合物介导的炎症。R406 还抑制 Lyn (IC₅₀=63 nM) 和 Lck (IC₅₀=37 nM).
生物活性	R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC 50 of 41 nM, measured at an ATP concentration corresponding to its K m value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC 50 =63 nM) and Lck (IC 50 =37 nM).
性状	Solid
IC50 & Target[1][2]	Ki: 30 nM (Syk) IC50: 41 nM (Syk) FLT3 IC50: 63 nM (Lyn), 37 nM (Lck)
体外研究(In Vitro)	R406 inhibits adenosine A3 receptor (IC50=0.081 μM), adenosine transporter (IC50=1.84 μM), and monoamine transporter (IC50=2.74 μM). R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 μM, respectively. R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. [2]. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8.

溶解度数据	In Vitro: DMSO : ≥ 61 mg/mL (97.04 mM)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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