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R406
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
R406图片
CAS NO:841290-81-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
R406 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 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 competitiveSyk/FLT3inhibitor for ATP binding with aKiof 30 nM, potently inhibitsSykkinase activity in vitro with anIC50of 41 nM, measured at an ATP concentration corresponding to its Kmvalue. R406 reduces immune complex-mediated inflammation[1]. R406 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].

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].

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

628.63

性状

Solid

Formula

C28H29FN6O8S

CAS 号

841290-81-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 61 mg/mL(97.04 mM)

H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5908 mL7.9538 mL15.9076 mL
5 mM0.3182 mL1.5908 mL3.1815 mL
10 mM0.1591 mL0.7954 mL1.5908 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ≥ 2.5 mg/mL (3.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.98 mM,饱和度未知) 的澄清溶液。

    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 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% (20%SBE-β-CDin saline)

    Solubility: 2.5 mg/mL (3.98 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (3.98 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。