Home Metabolism AhR antagonist BAY 2416964 For research use only.

BAY 2416964

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.

BAY 2416964 Chemical Structure

BAY 2416964 Chemical Structure

CAS: 2242464-44-2

Selleck's BAY 2416964 has been cited by 1 publication

Purity & Quality Control

Batch: S899501 DMSO] 78 mg/mL] false] Ethanol] 1.5 mg/mL] false] Water] Insoluble] false Purity: 99.80%
99.80

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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
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]
Cell Research 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).
In Vivo
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]
Animal Research Animal Models Female C57/BL6N mice with B16F10OVA tumor cells
Dosages 30 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04999202 Recruiting
Advanced Solid Tumors
Bayer
 August 30 2021 Phase 1
NCT04069026 Active not recruiting
Advanced Solid Tumors
Bayer
 August 15 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 387.82 Formula

C18H18ClN5O3
CAS No. 2242464-44-2 SDF --
Smiles CC(CO)NC(=O)C1=CC(=NN(C1=O)C2=CN(N=C2)C)C3=CC=C(C=C3)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 78 mg/mL ( (201.12 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1.5 mg/mL

Water : Insoluble


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In vivo
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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.

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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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