BAY-985

Product NameBAY-985
CAS2409479-29-2
MFC27H30F3N9O
MW553.58
EINECS
MOL File2409479-29-2.mol

Chemical Properties

Boiling point	753.3±70.0 °C(Predicted)
Density	1.373±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 50 mg/mL (90.32 mM)
form	A solid
pka	10.06±0.10(Predicted)
color	Light yellow to yellow

Usage And Synthesis

Biological Activity

BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. It is highly potent against TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε (IC50 = 2 nM) and also in mechanocellular phosphorylation of interferon regulatory factor 3 (pIRF3) assays High potency (IC50 = 74 nM) and anti-proliferative effect on SK-MEL-2 cells (IC50 = 900 nM).

in vitro

BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 with IC ₅₀ s of 123, 276, 311, and 7930 nM, respectively.
BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) with an IC ₅₀ of 74 nM.
BAY-985 is active in cellular mechanistic assay and shows anti-proliferative activity in a few cancer cells lines with IC ₅₀ s of 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells, respectively.

Cell Proliferation Assay

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Cell Line:	ACHN and SK-MEL-2 cell lines
Concentration:
Incubation Time:	96 hours
Result:	Inhibited proliferation i n SK-MEL2 and ACHN cells with IC ₅₀ s of 900 and 7260 nM, respectively.

in vivo

BAY-985 (200 mg/kg; po; bid; 111 days) results in weak antitumor efficacy.
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).

Animal Model:	Female NMRI nude mice bearing SK-MEL-2 human melanoma xenograft model
Dosage:	200 mg/kg
Administration:	Applied po; twice daily (bid) continuously 111 days
Result:	Treatment resulted in weak antitumor efficacy with a T/C _{tumor weight} ratio of 0.6. The treatment was well tolerated, with a maximum body weight loss of less than 10%.

target

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> TBK1
(in high ATP assay)

Target	Value
TBK1 (in low ATP assay)	2 nM
IKKε (Cell-free assay)	2 nM
30 nM
pIRF3 (Cell-free assay)	74 nM

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