1. NF-κB
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  3. BAY-985

BAY-985 

Cat. No.: HY-133117
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BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy.

For research use only. We do not sell to patients.

BAY-985 Chemical Structure

BAY-985 Chemical Structure

CAS No. : 2409479-29-2

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Description

BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy[1].

IC50 & Target[1]

TBK1

2 nM (IC50, low ATP)

TBK1

30 nM (IC50, high ATP)

IKKε

2 nM (IC50)

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].

Cell Proliferation Assay[1]

Cell Line: ACHN and SK-MEL-2 cell lines
Concentration:
Incubation Time: 96 hours
Result: Inhibited proliferation in SK-MEL2 and ACHN cells with IC50s of 900 and 7260 nM, respectively.
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 (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)[1].

Animal Model: Female NMRI nude mice bearing SK-MEL-2 human melanoma xenograft model[1]
Dosage: 200 mg/kg
Administration: Applied p.o.; twice daily (b.i.d.) continuously 111 days
Result: Treatment resulted in weak antitumor efficacy with a T/Ctumor weight ratio of 0.6.
The treatment was well tolerated, with a maximum body weight loss of less than 10%.
Molecular Weight

553.58

Formula

C₂₇H₃₀F₃N₉O

CAS No.

2409479-29-2

SMILES

O=C(N1CCN([[email protected]@H](C2=CC(NC3=NC4=CC=C(C5=NC=NC(N(C)C)=C5)C=C4N3)=NC=C2)C)CC1)CC(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BAY-985BAY985BAY 985IKKIκB kinaseI kappa B kinaseTBK1IKKεantitumormelanomaInhibitorinhibitorinhibit

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