Information BAY-218 BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. Targets AhR In vitro Mechanistically, BAY-218 inhibits AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. BAY-218 rescues TNFα production from kynurenic acid(KA)-suppressed LPS-treated primary human monocytes. In vivo BAY-218 enhances anti-tumoral immune responses and reduced tumor growth in the syngeneic mouse tumor models CT26 and B16-OVA. Furthermore, BAY-218 enhances therapeutic efficacy of an anti-PD-L1 antibody in the CT26 model.
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BAY-218
CAS number：2162982-11-6 molecular formula：C2OH17ClFN3O3
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| Chinese alias | - | ||
| English alias | AHR antagonist 1 | 6-(4-Chlorophenyl)-2-(3-fluorophenyl)-N-[(2S)-1-hydroxy-2-propanyl]-3-oxo-2,3-dihydro-4-pyridazinecarboxamide | ||
| CAS number | 2162982-11-6 | molecular formula | C2OH17ClFN3O3 |
| molecular weight | 401.82 g/mol | Exact mass | ≥99% |
| PSA | 82.000 Ų | logp | 3.106 |
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