BAY-2416964

BAY-2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY2416964 specifically binds to AhR, inhibits AhR activation, and prevents AhR-mediated signaling. Abrogation of AhR activation prevents the activation of immune-tolerant dendritic cells (DCs) and regulatory T cells (Tregs) in the tumor microenvironment (TME). This may restore the immune response against tumor cells. .

Product information

CAS Number: 2242464-44-2

Molecular Weight: 387.82

Formula: C18H18ClN5O3

Synonym:

BAY-2416964

BAY 2416964

BAY2416964

Chemical Name: (S)-6-(4-chlorophenyl)-N-(1-hydroxypropan-2-yl)-2-(1-methyl-1H-pyrazol-4-yl)-3-oxo-2,3-dihydropyridazine-4-carboxamide

Smiles: CN1C=C(C=N1)N1N=C(C=C(C(=O)N[C@@H](C)CO)C1=O)C1C=CC(Cl)=CC=1

InChiKey: YAGSZKAJPHGVOV-NSHDSACASA-N

InChi: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

BAY 2416964 (Example 192) induces AHR-regulated gene CYP1A1 expression in a human monocytic U937 cells with an IC50 of 4.3 nM.

References:

1. IlonaGUTCHER,etal.2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamides for the treatment of cancer. WO2018146010A1

Products are for research use only. Not for human use.