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R406 free base

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Chemical Structure| 841290-80-0 同义名 : R406;free base
CAS号 : 841290-80-0
货号 : A233735
分子式 : C22H23FN6O5
纯度 : 98%
分子量 : 470.454
MDL号 : MFCD09970820
存储条件:

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 25 mg/mL(53.14 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

1% DMSO+30% polyethylene glycol+1% Tween 80+water 30 mg/mL suspension

生物活性
描述 R406 is a potent Syk inhibitor with IC50 of 41 nM that strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01725230 Rheumatoid Arthritis Phase 1 Completed - United States, Kansas ... 展开 >> Research Site Overland Park, Kansas, United States 收起 <<
NCT01208155 Bioavailability ... 展开 >> Pharmacokinetics 收起 << Phase 1 Completed - United States, Kansas ... 展开 >> Research Site Overland Park, Kansas, United States 收起 <<
NCT01245790 Rheumatoid Arthritis ... 展开 >> Renal Impairment 收起 << Phase 1 Completed - United States, Florida ... 展开 >> Research Site Orlando, Florida, United States 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.63mL

2.13mL

1.06mL

21.26mL

4.25mL

2.13mL

参考文献

[1]Chen L, Monti S, et al. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood. 2008 Feb 15;111(4):2230-7.

[2]Braselmann S, Taylor V, 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.