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Biological Activity:
Orally bioavailable and selective inhibitor of spleen tyrosine kinase (Sky) (Ki=30 nM). Active component of its prodrug R788 or R935788 (Fostamatinib).
References:
S 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, 319(3), 998-1008. [online]
HS 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, 317(2), 571-578. [online]
JC Spalton et al. The novel Syk inhibitor R406 reveals mechanistic differences in the initiation of GPVI and CLEC-2 signaling in platelets. J. Thromb. Haemost. 2009, 7, 1-8. [online]
Chemical Name: 6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
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