BAY 2416964

Catalog No.S8995 Batch:S899501

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Technical Data

Formula

C18H18ClN5O3
Molecular Weight 387.82 CAS No. 2242464-44-2
Solubility (25°C)* In vitro DMSO 78 mg/mL (201.12 mM)
Ethanol 1.5 mg/mL (3.86 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.9mg/ml
5% DMSO 95% Corn oil
1.9mg/ml
* <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 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors.
Targets
AhR [1]
(Cell-free assay)
341 nM
In vitro

BAY 2416964 (Example 192) induces AHR-regulated gene CYP1A1 expression with IC50 of 4.30 nM in a human monocytic U937 cells.[1]
In vivo

In vivo assays: BAY 2416964 (Example 192) is dissolved in Ethanol/Solutol/Water (10/40/50) and given at 30 mg/kg, QD, p.o.. The efficacy is calculated based on tumor volume. BAY 2416964 (Example 192) is shown to have the potential for solid tumour treatment.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    human monocytic U937 cell line

  • Concentrations

    3.1 nmol/L, 11 nmol/L, 38 nmol/L, 130 nmol/L, 470 nmol/L, 1.6 pmol/L, 5.7 pmol/L and 20 pmol/L

  • Incubation Time

    20 h

  • Method

    Cells in medium (tryptophan free RPMI, 1% FCS, 2mM Glutamine) supplemented with 150 μM kynurenic acid are grown for 20 hours in absence (negative control) or presence of increasing concentrations of BAY 2416964 (typical dilutions: 72 pmol/L, 0.25 nmol/L, 0.89 nmol/L; 3.1 nmol/L, 11 nmol/L, 38 nmol/L, 130 nmol/L, 470 nmol/L, 1.6 pmol/L, 5.7 pmol/L and 20 pmol/L in duplicates).
Animal Study:

[1]
  • Animal Models

    Female C57/BL6N mice with B16F10OVA tumor cells

  • Dosages

    30 mg/kg

  • Administration

    Oral gavage

Selleck's BAY 2416964 has been cited by 2 publications

Aryl hydrocarbon receptor restricts axon regeneration of DRG neurons in response to injury [ bioRxiv, 2024, 2023.11.04.565649] PubMed: 37961567
Tubular aryl hydratocarbon receptor upregulates EZH2 to promote cellular senescence in cisplatin-induced acute kidney injury [ Cell Death Dis, 2023, 14(1):18] PubMed: 36635272

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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.