BAY-985

Catalog No.S8935

For research use only.

BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM).

BAY-985 Chemical Structure

CAS No. 2409479-29-2

Purity & Quality Control

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Biological Activity

Description BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM).
Targets
TBK1 [1]
(in low ATP assay)
IKKε [1]
(Cell-free assay)
TBK1 [1]
(in high ATP assay)
pIRF3 [1]
(Cell-free assay)
2 nM 2 nM 30 nM 74 nM
In vitro

BAY-985 is a potent and highly selective TBK1/IKKε inhibitor that inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2.[1]

In vivo

BAY-985 shows only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model.[1]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: ACHN, SK-MEL-2, MDA-MB231 cells
  • Concentrations: 100 nM
  • Incubation Time: 96 h
  • Method:

    For proliferation assays, cells are plated in white 384-well microtiter plates at 300 (ACHN) and 800 (SK-MEL-2) cells/well, respectively, in 50 μL medium. The following day, BAY-985 is added to the cells using a D300 Digital Dispenser. After 96 h, cell numbers are determined using CellTiter-Glo solution. Luminescence is read on a VICTOR reader. The luminescence signal is compared to the signal measured on sister plates on the day of compound addition (time zero).

Animal Research:

[1]

  • Animal Models: male Wistar rats; female NMRI nude mice
  • Dosages: 0.30 mg/kg; 100 mg/kg
  • Administration: IV, Oral gavage

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(180.64 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 553.58
Formula

C27H30F3N9O

CAS No. 2409479-29-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC(=NC=C1)NC2=NC3=C(N2)C=C(C=C3)C4=CC(=NC=N4)N(C)C)N5CCN(CC5)C(=O)CC(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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