An AhR antagonist
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BAY-2416964

Item No. 36939

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(4-chlorophenyl)-2,3-dihydro-N-[(1S)-2-hydroxy-1-methylethyl]-2-(1-methyl-1H-pyrazol-4-yl)-3-oxo-4-pyridazinecarboxamide
CAS Number
2242464-44-2
Molecular Formula
C18H18ClN5O3
Formula Weight
387.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1N(C2=CN(C)N=C2)N=C(C3=CC=C(C=C3)Cl)C=C1C(N[C@@H](C)CO)=O
InChi Code
InChI=1S/C18H18ClN5O3/c1-11(10-25)21-17(26)15-7-16(12-3-5-13(19)6-4-12)22-24(18(15)27)14-8-20-23(2)9-14/h3-9,11,25H,10H2,1-2H3,(H,21,26)/t11-/m0/s1
InChi Key
YAGSZKAJPHGVOV-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $65

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    10 mg

    $117

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    25 mg

    $260

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    50 mg

    $455

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    Cayman Chemical
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    Product Description

    BAY-2416964 is an antagonist of the aryl hydrocarbon receptor (AhR; IC50 = 22 nM in U87 cells).1 It decreases the mRNA expression of the AhR target genes CYP1A1 and AHRR induced by the AhR agonist kynurenic acid (Item No. 16792) in LPS-stimulated isolated human monocytes when used at a concentration of 100 nM. BAY-2416964 (30-1,000 nM) increases CD3-, CD28-, and IL-2-induced IFN-γ production in isolated human naïve CD4+ T cells. In vivo, BAY-2416964 (30 mg/kg, p.o.) reduces tumor volume, increases CD8+ T cell and natural killer (NK) cell tumor infiltration, and decreases GR1+ myeloid cell and CD206+ M2 macrophage tumor infiltration in a B16/F10-OVA murine melanoma model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kober, C., Roewe, J., Schmees, N., et al. Targeting the aryl hydrocarbon receptor (AhR) with BAY 2416964: A selective small molecule inhibitor for cancer immunotherapy. J. Immunother. Cancer 11(11), e007495 (2023).