BAY-985

Catalog No.S8935 Batch:S893501

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Technical Data

Formula

C27H30F3N9O
Molecular Weight 553.58 CAS No. 2409479-29-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (180.64 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:

[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 Study:

[1]
  • Animal Models

    male Wistar rats; female NMRI nude mice

  • Dosages

    0.30 mg/kg; 100 mg/kg

  • Administration

    IV, Oral gavage

Selleck's BAY-985 has been cited by 3 publications

Executioner caspases restrict mitochondrial RNA-driven Type I IFN induction during chemotherapy-induced apoptosis [ Nat Commun, 2023, 14(1):1399] PubMed: 36918588
Executioner caspases restrict mitochondrial RNA-driven Type I IFN induction during chemotherapy-induced apoptosis [ Nat Commun, 2023, 14(1):1399] PubMed: 36918588
The m6A demethylase ALKBH5 promotes tumor progression by inhibiting RIG-I expression and interferon alpha production through the IKKε/TBK1/IRF3 pathway in head and neck squamous cell carcinoma [ Mol Cancer, 2022, 21(1):97] PubMed: 35395767

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.