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R406

产品编号 T6174 CAS 841290-81-1

别名: R-406 besylate

R406 (R-406 besylate) 是一种具有口服活性的 ATP 竞争性 Syk/FLT3抑制剂，Ki 为 30 nM。它有效抑制 Syk 激酶活性，IC50为 41 nM。它还抑制 Lyn 和 Lck，IC50值分别为 63 nM 和 37 nM。它可减轻免疫复合物介导的炎症。

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R406, CAS 841290-81-1

规格	价格/CNY	货期
1 mg	￥ 459	现货
2 mg	￥ 669	现货
5 mg	￥ 987	现货
10 mg	￥ 1,650	现货
25 mg	￥ 2,850	现货
50 mg	￥ 4,220	现货
100 mg	￥ 5,900	现货
1 mL * 10 mM (in DMSO)	￥ 1,310	现货

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其他形式的 R406:

R406 free base
现货

选择批次

纯度: 98.82%

纯度: 97.67%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	R406 (R-406 besylate) is an effective Syk inhibitor (IC50: 41 nM) and shows no effects on Lyn.
靶点活性	Syk:30 nM (Ki, cell free), Syk:41 nM (Ki, cell free)
体外活性	R406 dose-dependently inhibited anti-IgE-mediated CHMC degranulation measured as tryptase release (EC50: 0.056 μM) but showed no activity on ionomycin-triggered tryptase release. R406 also inhibited the anti-IgE induced production and release of LTC4 and cytokines and chemokines, including TNF, IL-8, and GM-CSF. R406 potently inhibited Syk kinase activity in vitro with an IC50 of 41 nM. Subsequent enzyme kinetic studies showed R406 to be a competitive inhibitor for ATP binding with a Ki of 30 nM [1]. R406 induces apoptosis and cell cycle arrest while decreasing downstream phosphatidylinositol-3'-kinase (PI3K)/Akt signaling in EBV+ B cell lymphoma PTLD lines in vitro [2]. The prosurvival effects promoted by anti-IgM stimulation and nurselike cells were abrogated by R406. BCR triggering up-regulated adhesion molecules and increased CLL cell migration toward the chemokines CXCL12 and CXCL13. BCR activation also enhanced CLL cell migration beneath marrow stromal cells. These responses were blocked by R406, which furthermore abrogated BCR-dependent secretion of T-cell chemokines (CCL3 and CCL4) by CLL cells [3].
体内活性	Prophylactic treatment of mice with R406 administered 1 h before immune complex challenge reduced the cutaneous reverse passive Arthus reaction by approximately 72 and 86% at 1 and 5 mg/kg, respectively, compared with the vehicle control. The net optical density reading of extravasated dye extracted after treatment with R406 at 1 or 5 mg/kg R406 was reduced from 0.14 (vehicle) to 0.04 or 0.02, respectively. Treatment of injected C57BL/6 mice with 10 mg/kg R406 bid delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50% [1]. R406 did not inhibit or delay the in vivo growth of solid tumors established from EBV-infected B cell lines. Instead, tumor growth in adjacent inguinal lymph nodes was observed exclusively in fostamatinib (R406 prodrug)-treated animals [2].
激酶实验	The fluorescence polarization reactions were performed as described elsewhere. For Ki determination, duplicate 200-μl reactions were set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R406 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μl of each reaction was removed and quenched to stop the reaction. For each concentration of R406, the rate of reaction at each concentration of ATP was determined and plotted against the ATP concentration to determine the apparent Km and Vmax (maximal rate). Finally, the apparent Km (or apparent Km/Vmax) was plotted against the inhibitor concentration to determine the Ki. All data analysis was performed using Prism and Prism enzyme kinetics programs [1].
细胞实验	Human primary macrophages were derived from CD14 peripheral blood mononuclear cell according to the protocol specified in the monocyte isolation kit and by subsequently expanding the monocytes in 100 ng/ml human GM-CSF for 5 days to drive differentiation to macrophages. THP-1 cells were primed with 10 ng/ml IFN-γ for 6 days before stimulation. Monocyte-derived macrophages were stimulated by immobilized (plate-bound) human IgG. R406 and 15,000 cells were added to the IgG-coated wells and incubated for 16 to 20 h at 37°C. LPS was used at a final concentration of 10 ng/ml in uncoated wells. TNF concentration in the supernatants was measured by Luminex assay [1].
动物实验	Mice were challenged intravenously with 1% ovalbumin (OVA) in saline (10 mg/kg) containing 1% Evans blue dye. Ten minutes later, mice were anesthetized with isofluorane and shaved dorsolaterally. The rabbit anti-OVA IgG (50 μg/25 μl) was injected intradermally on the left side of the back at three adjacent locations. Three injections of rabbit polyclonal IgG (50 μg/25 μl) on the opposite side of the same animal served as controls. R406 or vehicle (67% PEG 400) was administered to animals 60 min before antibody/antigen challenge. Four hours after challenge, the animals were euthanized, and skin tissue was assessed for edema and inflammation by measuring dye extravasation into the surrounding tissue. Punch biopsy of the injection sites (8 mm) were incubated in 2 ml of formamide at 80°C overnight. The concentration of the extravasated Evans blue dye was measured spectrophotometrically at OD610 [1].

别名	R-406 besylate
分子量	628.63
分子式	C22H23FN6O5·C6H6O3S
CAS No.	841290-81-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 8 mg/mL (12.72 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 100 mg/mL (159.08 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.5908 mL	7.9538 mL	15.9076 mL	39.769 mL
	5 mM	0.3182 mL	1.5908 mL	3.1815 mL	7.9538 mL
	10 mM	0.1591 mL	0.7954 mL	1.5908 mL	3.9769 mL
DMSO	20 mM	0.0795 mL	0.3977 mL	0.7954 mL	1.9885 mL
	50 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7954 mL
	100 mM	0.0159 mL	0.0795 mL	0.1591 mL	0.3977 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Braselmann S, 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, 319(3), 998-1008. 2. Hatton O, et al. Syk-induced phosphatidylinositol-3-kinase activation in Epstein-Barr virus posttransplant lymphoproliferative disorder. Am J Transplant. 2013 Apr;13(4):883-90. 3. Quiroga MP, et al. B-cell antigen receptor signaling enhances chronic lymphocytic leukemia cell migration and survival: specific targeting with a novel spleen tyrosine kinase inhibitor, R406. Blood. 2009 Jul 30;114(5):1029-37.

文献引用

1. Li L, Xu X, Lv K, et al. Asebogenin Suppresses Thrombus Formation via Inhibition of Syk Phosphorylation. British Journal of Pharmacology. 2022 2. Zhu Y, Gu H, Yang L, et al. Involvement of MST1/mTORC1/STAT1 activity in the regulation of B-cell receptor signalling by chemokine receptor 2. Clinical and Translational Medicine. 2022, 12(7): e887.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

R406 841290-81-1 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FLT Syk Spleen tyrosine kinase Fms like tyrosine kinase 3 FLT3 inhibit CD135 Inhibitor Cluster of differentiation antigen 135 R-406 R-406 besylate R 406 inhibitor

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R406

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords