Fostamatinib

产品说明书

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Chemical Structure| 901119-35-5 同义名 : R788
CAS号 : 901119-35-5
货号 : A115345
分子式 : C23H26FN6O9P
纯度 : 99%+
分子量 : 580.46
MDL号 : MFCD16628163
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(103.37 mM)，配合低频超声助溶，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
生物活性
靶点

  • Syk

    Syk, IC50:41 nM
描述 Fostamatinib (R788) serves as the oral prodrug of the active compound R406 [1]. R406, an orally active and competitive inhibitor of Syk/FLT3, possesses a Ki of 30 nM and an IC50 of 41 nM[2]. R406 additionally demonstrates inhibition of Lyn (IC50=63 nM) and Lck (IC50=37 nM) [3].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human Ramos cells Function assay Inhibition of SYK in human Ramos cells, IC50=0.267 μM 23350847
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.61mL

1.72mL

0.86mL

17.23mL

3.45mL

1.72mL
参考文献

[1]Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273.

[2]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.

[3]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.