BAY 2416964

For research use only.

Catalog No.S8995

BAY 2416964 Chemical Structure

CAS No. 2242464-44-2

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.

Purity & Quality Control

Choose Selective AhR Inhibitors

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

Cell Research:

[1]

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  • 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).


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female C57/BL6N mice with B16F10OVA tumor cells
  • Dosages: 30 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (201.12 mM)
Ethanol 1.5 mg/mL (3.86 mM)
Water 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.

Chemical Information

Molecular Weight 387.82
Formula

C18H18ClN5O3

CAS No. 2242464-44-2
Storage powder
in solvent
Synonyms N/A
Smiles CC(CO)NC(=O)C1=CC(=NN(C1=O)C2=CN(N=C2)C)C3=CC=C(C=C3)Cl

In vivo Formulation Calculator (Clear solution)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04999202 Recruiting Drug: BAY2416964|Drug: Pembrolizumab Advanced Solid Tumors Bayer August 30 2021 Phase 1
NCT04069026 Recruiting Drug: BAY2416964 Advanced Solid Tumors Bayer August 15 2019 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID