BAY 2416964

SKU: orb1310013

Description

BAY 2416964 is a potent and selective aryl hydrocarbon receptor (AhR) inhibitor with an IC50 of 341 nM. This small molecule tool compound is widely utilized in immuno-oncology research to investigate AhR's role in modulating immune responses, both in cellular assays and in vivo models.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 2242464-44-2
• MW: 387.82
• Purity: 99.88%
• Formula: C₁₈H₁₈ClN₅O₃
• SMILES: C[C@@H](CO)NC(=O)c1cc(nn(-c2cnn(C)c2)c1=O)-c1ccc(Cl)cc1
• Target: Aryl Hydrocarbon Receptor
• Solubility: DMSO:64.4 mg/mL (166.06 mM)

Bioactivity

• Target IC50:
  CYP1A1:4.3 nM|AhR:341 nM|AHR (U87 cells):22 nM
• In Vivo:
  METHODS: To assay antitumor activity in vivo, BAY 2416964 (30 mg/kg) was administered orally to NSG mice bearing B16F10-OVA tumors once daily for seven days. RESULTS: BAY 2416964 inhibited tumor growth.BAY 2416964 increased the frequency of immunostimulatory tumor-infiltrating CD8+ T cells and N cells, and decreased the frequency of immunosuppressive GR1-positive myeloid cells and CD206+M2 macrophages.
• In Vitro:
  METHODS: Human monocytes were treated with BAY 2416964 (1 nM-10 µM), kynurenic acid (200 µM), and LPS (10 ng/mL) for 24 h, and TNF-α levels were measured by ELISA. RESULTS: kynurenic acid-induced AhR activation inhibited TNF-α production in LPS-stimulated monocytes, and BAY 2416964 dose-dependently rescued this AhR-mediated inhibition.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CYP1A1, AhR, BAY 2416964, BAY2416964, BAY-2416964, Aryl hydrocarbon receptor, Aryl Hydrocarbon Receptor, ArylHydrocarbonReceptor, anti-cancer, Inhibitor, inhibit

Compound Identifiers

PubChem CID

135303769