TAS05567 (TAS-5567) is a novel potent, selective, orally available Spleen tyrosine kinase (Syk) inhibitor with IC50 of 0.37 nM.
TAS05567 shows >70% inhibition of Syk and 4 other kinases in a panel of 192 kinases, more selective and potent than R406.
TAS05567 suppresses induction of BLNK phosphorylation by anti-IgM in Ramos cells (IC50=1.8 nM).
TAS05567 inhibits BCR-dependent signal transduction in Ramos cells, FcγR-mediated TNF-α production in THP-1 cells, and FcεR-mediated histamine release from RBL-2H3 cells.
TAS05567 suppresses hind-paw swelling in a dose-dependent manner, markedly reduces histopathologic scores in rheumatoid arthritis models.
