RO9021 是口服具有活力的，ATP 竞争性的Syk抑制剂，其IC50=5.6 nM。

RO9021 is an orally bioavailable, novel ATP-competitive SYK inhibitor (average IC50: 5.6 nM).

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 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 also shows a similar inhibitory potency (IC50=22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay [1].

1446790-62-0

C18H25N7O

355.44

DMSO:3 mg/mL (8.44 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years