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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $175 | In Stock | |
5 mg | $372 | In Stock | |
10 mg | $597 | In Stock | |
25 mg | $953 | In Stock | |
50 mg | $1,290 | In Stock | |
100 mg | $1,730 | In Stock | |
1 mL x 10 mM (in DMSO) | $453 | In Stock |
Description | 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. |
Targets&IC50 | TBK1:2 nM (low ATP), TBK1:30 nM (high ATP), IKKε:2 nM |
In vitro | 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). |
In vivo | 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). |
Molecular Weight | 553.58 |
Formula | C27H30F3N9O |
Cas No. | 2409479-29-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (90.32 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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