BAY-985

2409479-29-2

553.58

DMSO : 50 mg/mL (90.32 mM; Need ultrasonic)

NF-kappaB

BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKepsilon with IC₅₀s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKepsilon, respectively. Antitumor efficacy^[1]. In Vitro: BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 with IC₅₀s of 123, 276, 311, and 7930 nM, respectively^[1].
BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) with an IC₅₀ of 74 nM^[1].
BAY-985 is active in cellular mechanistic assay and shows anti-proliferative activity in a few cancer cell lines with IC₅₀s of 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells, respectively^[1]. In Vivo: BAY-985 (200 mg/kg; p.o.; b.i.d.; 111 days) results in weak antitumor efficacy^[1].
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)^[1].