Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC50 of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers.IC50 & Target: IC50: 0.31 nM (SYK)In Vitro: Syk-IN-4 is a potent inhibitor of hERG with an IC50 of 3.0 μM.
Syk-IN-4 inhibits SUDHL-4 and T cell proliferation with GI50s of 0.24 and 2.6 μM, respectively.In Vivo: Syk-IN-4 exhibits moderate oral bioavailability (60%) following oral administration (1 mg/kg) in male Hans Wistar rats.
Syk-IN-4 exhibits high plasma clearance (151 mL/min/kg) combined with large volumes of distribution (1.0 L/kg respectively) following i.v. administration (0.5 mg/kg) in male Hans Wistar rats.