Biological Activity
BAY 61-3606 (dihydrochloride) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase (IC50=10 nM) with no inhibitory effect on Btk, Fyn, Itk, Lyn, and Src.
In Vitro
BAY 61-3606 inhibits the release of various inflammatory mediators in a concentration-dependent manner. The IC50 values for the FcϵRI-mediated hexosaminidase release from a rat basophilic leukemia cell line, RBL-2H3, and serotonin release from rat peritoneal mast cells are found to be 46 and 17 nM, respectively. BAY 61-3606 inhibits FcϵRI-mediated histamine and tryptase release from HCMCs with IC50 values of 5.1 and 5.5 nM, respectively, in a manner similar to its effect on the degranulation of RBL-2H3 cells and rat peritoneal mast cells. BAY 61-3606 inhibits histamine release from leukocytes in high and low IgE groups equipotently, giving IC50 values of 8.1 and 10 nM, respectively[1]. BAY 61-3606 affects viability in cells expressing mutant K-RAS or B-RAF through a MAPK-independent pathway. Inhibition of SYK is not responsible for the BAY 61-3606 effect on cell viability in colorectal cancer cells. MAP4K2 is a target for BAY 61-3606 that modulates the response of wild-type cells to AZ-628[2]. BAY61-3606 has a 50% Cytotoxicity Concentration (CC50) value of greater than 100 μM, and it inhibits AD169 replication[3].
In Vivo
BAY 61-3606 (3, 10, 30, 100 mg/kg, p.o.) dose dependently inhibits the PCA reaction with an ED50 value of 8 mg/kg. In a bronchoconstriction model, BAY 61-3606 dose dependently inhibits the DNP-BSA-induced increase in pulmonary pressure, and the dose of 3 mg/kg shows statistically significant suppression[1].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.