BAY-218

Alias: BAY2335218; BAY218; BAY-2335218; BAY 218; BAY 2335218; BAY-218;
Cat No.:V4433 Purity: ≥98%
BAY-218 (BAY218) is a novel, potent and selective small-molecule AhR (aryl hydrocarbon receptor) inhibitor with anticancer activities.
BAY-218 Chemical Structure CAS No.: 2162982-11-6
Product category: AhR
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

BAY-218 (BAY218) is a novel, potent and selective small-molecule AhR (aryl hydrocarbon receptor) inhibitor with anticancer activities. It is used as a new modality to counteract tumor immunosuppression.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
BAY-218 (Example 23) (72 pM – 20 μM) inhibits AHR in U87 astrocytes, with an IC50 of 39.9 μM [1]. CYP1A1 is inhibited by BAY-218 (1 nM–3 μM). The suppression of TNFα generation by LPS-stimulated human monocytes caused by KA is reversed by BAY-218 (1 μM) [1]. For the human monocyte U937 cell line, the activity, IC50 is 70.7 μM[1].
ln Vivo
Combining BAY-218 (Example 23) with aPD-L1 (oral 30 mg/kg; bid) provides good anti-tumor effects [1].
Cell Assay
RT-PCR[1]
Cell Types: Human monocytes U937 Cell
Tested Concentrations: 1 nM-3 μM
Incubation Duration:
Experimental Results: Regulation of antagonistic ligand-induced AHR genes in a dose-dependent manner.
Animal Protocol
Animal/Disease Models: balb/c (Bagg ALBino) mouse (subcutaneousCT26 cells) [1]
Doses: 30 mg/kg
Route of Administration: Orally, twice (two times) daily
Experimental Results: In combination with aPD-L1, tumor size was Dramatically diminished.
References
[1]. Norbert Schmees, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides. WO2017202816A1.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H17CLFN3O3
Molecular Weight
401.818687200546
CAS #
2162982-11-6
SMILES
O=C(C1=CC(C2=CC=C(Cl)C=C2)=NN(C3=CC=CC(F)=C3)C1=O)N[C@@H](C)CO
InChi Key
RFGRNBWAUZSMBN-LBPRGKRZSA-N
InChi Code
InChI=1S/C20H17ClFN3O3/c1-12(11-26)23-19(27)17-10-18(13-5-7-14(21)8-6-13)24-25(20(17)28)16-4-2-3-15(22)9-16/h2-10,12,26H,11H2,1H3,(H,23,27)/t12-/m0/s1
Chemical Name
(S)-6-(4-chlorophenyl)-2-(3-fluorophenyl)-N-(1-hydroxypropan-2-yl)-3-oxo-2,3-dihydropyridazine-4-carboxamide
Synonyms
BAY2335218; BAY218; BAY-2335218; BAY 218; BAY 2335218; BAY-218;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 250 mg/mL (~622.17 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4887 mL 12.4434 mL 24.8868 mL
5 mM 0.4977 mL 2.4887 mL 4.9774 mL
10 mM 0.2489 mL 1.2443 mL 2.4887 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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