R406 free base

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

R406 free base  纯度: 99.69%

R406 free base 是一种有效的，具有口服活性的，ATP竞争性的 Syk/FLT3 抑制剂，Ki 为 30 nM，有效抑制 Syk 激酶活性，IC50 为 41 nM。R406 free base 可减轻免疫复合物介导的炎症。R406 free base 还抑制 Lyn (IC50=63 nM) 和 Lck (IC50=37 nM).

R406 free base

R406 free base Chemical Structure

CAS No. : 841290-80-0

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1729 In-stock
2 mg ￥810 In-stock
5 mg ￥1250 In-stock
10 mg ￥1989 In-stock
50 mg ￥6412 In-stock
100 mg ￥10114 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

R406 free base 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Diabetes Related Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation[1]. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2].

IC50 & Target

Ki: 30 nM (Syk)[1]
IC50: 41 nM (Syk)[1]
FLT3[1]
IC50: 63 nM (Lyn), 37 nM (Lck)[2]
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)[1].
R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 µM, respectively[1].
R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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[1].

上海金畔生物科技有限公司 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[1]
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[1]
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%.

分子量

470.45

Formula

C22H23FN6O5
CAS 号

841290-80-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 10 mg/mL (21.26 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.5 mg/mL (1.06 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (1.06 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.0 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 ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.5 mg/mL (1.06 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (1.06 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 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务