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Fostamatinib

Chemical Structure : Fostamatinib

CAS No.: 901119-35-5

Fostamatinib (R788, R-788)

Catalog No.: PC-43349Not For Human Use, Lab Use Only.

Fostamatinib (R788) is a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Fostamatinib (R788) is a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41 nM。
Fostamatinib (R788) dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM, inhibits all phosphorylation events downstream of Syk signaling。
Fostamatinib (R788) specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils. R788 can inhibit local inflammatory injury mediated by immune complexes。
Fostamatinib (R788) reduces immune complex-mediated inflammation in arthritis models.

Physicochemical Properties

M.Wt 580.4595
Formula C23H26FN6O9P
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one, 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl-4-[(phosphonooxy)methyl]-

References

1. Braselmann S, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

2. Chen L, et al. Blood. 2008 Feb 15;111(4):2230-7.

3. Suljagic M, et al. Blood. 2010 Dec 2;116(23):4894-905.

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