BAY-985

BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 with IC ₅₀ s of 123, 276, 311, and 7930 nM, respectively.
BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) with an IC ₅₀ of 74 nM.
BAY-985 is active in cellular mechanistic assay and shows anti-proliferative activity in a few cancer cells lines with IC ₅₀ s of 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells, respectively.

BAY-985 (200 mg/kg; po; bid; 111 days) results in weak antitumor efficacy.
BAY-985 shows high clearance (CL _b = 4.0 L/h/kg, ca. 95% hepatic extraction), large volume of distribution at steady state (V _ss =2.9 L/kg) and a short terminal half-life (t _{1 /2} =0.79 h).