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BAY-985

Catalog No. T10477   CAS 2409479-29-2

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.

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BAY-985 Chemical Structure
BAY-985, CAS 2409479-29-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 175.00
5 mg In stock $ 372.00
10 mg In stock $ 597.00
25 mg In stock $ 953.00
50 mg In stock $ 1,290.00
100 mg In stock $ 1,730.00
1 mL * 10 mM (in DMSO) In stock $ 453.00
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Purity: 99.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Solubility Information

DMSO: 50 mg/mL (90.32 mM), sonification is recommended.

TargetMolReferences and Literature

1. Lefranc J, et al. Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor. J Med Chem. 2020 Jan 10.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Antidepressant Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Bioactive Compound Library Anti-Ovarian Cancer Compound Library Pyroptosis Compound Library Immunology/Inflammation Compound Library Orally Active Compound Library

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Keywords

BAY-985 2409479-29-2 NF-Κb IκB/IKK BAY 985 BAY985 IKK IκB kinase melanoma IKKε TBK1 inhibit I kappa B kinase Inhibitor antitumor inhibitor

 

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