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RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC₅₀ of 5.6 nM.

RO9021 is a highly selective SYK inhibitor with low S-scores of 0.003 for S(99) and 0.015 for S(90), indicating that SYK is the only kinase with 99% competition with RO9021 in a total of 392 tested kinases. RO9021 inhibits anti-IgM induced phosphorylation of BTK, PLCγ2, AKT and ERK, indicating that blockade of SYK kinase activity by RO9021 results in attenuation of BCR downstream signaling cascade. RO9021 selectively suppresses B-cell receptor signaling. RO9021 also displays a similar inhibitory potency (IC₅₀=22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay.

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