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R406 (free base)

Syk抑制剂，R406是Syk抑制剂，IC50为41 nM，对Lyn活性较弱。

目录号: PC16061 纯度: ≥98%

CAS No. :841290-80-0

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PC16061-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1813.00	请登录

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中文名称

R406 (free base)

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-噁嗪-3(4H)-酮;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;6 - （5 - 氟 - 2 - （3,4,5 - 三甲氧基苯基氨基）-4 - 基氨基）-2-嘧啶,;R-406

英文名称

R406 (free base)

英文别名

R-406;6-[5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one;6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one;6-[5-Fluoro-2-(3,4,5-trimethoxy-phenylamino)-pyrimidin-4-ylamino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one;R406 (free base);R406;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-;6-(5-Fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one;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;6-[[5-Fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one ;R406 Free base;compound 1007;N4-aminocytidine minimum;N4-NH2-Cr;N-Aminocytidine;uridine,4-hydrazone

Cas No.

841290-80-0

分子式

C₂₂H₂₃N₆O₅F

分子量

470.45

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity 体外研究 with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	Cultured human mast cells (CHMC)
Concentration:	0.016, 0.08, 0.4, 2 μM
Incubation Time:	40 minutes
Result:	Inhibited all other kinases tested at 5 to 100 fold less potency than Syk as judged by phosphorylation of target proteins.

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c mice (6-8 weeks) with CAIA
Dosage:	5 and 10 mg/kg
Administration:	Administered orally, b.i.d, for 14 days, starting 4 hours after antibody challenge on day 0.
Result:	Reduced inflammation and swelling, and the arthritis progressed more slowly in treated animals than in vehicle controls.

Animal Model:	Female C57BL/6 mice with arthritis
Dosage:	10 mg/kg
Administration:	Administered orally one hour before serum injection; b.i.d; for 13 days
Result:	Delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50%.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 25 mg/mL (53.14 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1256 mL	10.6281 mL	21.2562 mL
5 mM	0.4251 mL	2.1256 mL	4.2512 mL
10 mM	0.2126 mL	1.0628 mL	2.1256 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (5.31 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.31 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.31 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

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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