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[1].
Syk-IN-4 is a potent inhibitor of hERG with an IC50 of 3.0 μM[1].Syk-IN-4 inhibits SUDHL-4 and T cell proliferation with GI50s of 0.24 and 2.6 µM, respectively[1].
Syk-IN-4 exhibits moderate oral bioavailability (60%) following oral administration (1 mg/kg) in male Hans Wistar rats[1]. 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[1].
[1]. Neil P Grimster, et al. Optimization of a Series of Potent, Selective and Orally Bioavailable SYK Inhibitors. Bioorg Med Chem Lett. 2020 Jul 24;127433.