BAY-985 是高效的、ATP 竞争性的、有口服活性的、选择性的TBK1和IKKε双重抑制剂，对 TBK1 (在低/高 ATP 实验中) 和 IKKε 的IC50分别为 2/30 和 2 nM。它具有抗肿瘤作用。

BAY-985 is a potent, selective, and orally active ATP-competitive dual inhibitor of TBK1 and IKKε (IC50s: 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε) with antitumor efficacy.

BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 (IC50s: 123, 276, 311, and 7930 nM). BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3, IC50: 74 nM). BAY-985 shows anti-proliferative activity in a few cancer cell lines (IC50s: 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells).

BAY-985 (200 mg/kg; p.o.; b.i.d.; 111 days) results in weak antitumor efficacy. BAY-985 shows high clearance (CLb= 4.0 L/h/kg, ca. 95% hepatic extraction), large volume of distribution at steady state (Vss=2.9 L/kg) and a short terminal half-life (t1/2=0.79 h).

2409479-29-2

C27H30F3N9O

553.58

DMSO:50 mg/mL (90.32 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years