BAY-218 free base · Synonyms: AHR antagonist 1

BAY-218 is an aryl hydrocarbon receptor antagonist.

For research use only. Not for human or veterinary use.

Target Aryl Hydrocarbon Receptor

Research area Inflammation/Immunology Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

BAY-218 structure

CAS No.: 2162982-11-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 420.00	BP-01978-250mg	In stock	Get quote
500 mg	USD 608.00	BP-01978-500mg	In stock	Get quote
1 g	USD 882.00	BP-01978-1g	In stock	Get quote
5 g	Inquire	BP-01978-5g	Inquire	Inquire

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Description

BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses.

Biological activity

In Vitro BAY-218 (example 23) (72 pM-20 μM) has AHR inhibitory activity with an IC50 of 39.9 μM in in U87 glioblastoma cells. ? BAY-218 (1 nM-3 μM) has CYP1A1 inhibitory activity with an IC50 of 70.7 μM in human monocytic U937 cell line. ? BAY-218 (1 μM) reverses KA-induced inhibition of TNFα production by LPS stimulated human monocytes. In Vivo BAY-218 (example 23) (p.o; 30 mg/kg; bid) has good anti-tumor effect combinated with aPD-L1.

Identifiers

SMILES: O=C(C1=CC(C2=CC=C(Cl)C=C2)=NN(C3=CC=CC(F)=C3)C1=O)N[C@@H](C)CO
InChIKey: RFGRNBWAUZSMBN-LBPRGKRZSA-N

Specifications

MW (average): 401.8190
Formula: C₂₀H₁₇ClFN₃O₃
CAS No.: 2162982-11-6
Physical state: Solid
Color: light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Ilona Gutcher, Christina Kober, Lars Roese,et al.Abstract 1288: Blocking tumor-associated immune suppression with BAY-218, a novel, selective aryl hydrocarbon receptor (AhR) inhibitor[J].10.1158/1538-7445.AM2019-1288 Published July 2019.

[2]. Norbert Schmees, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides. WO2017202816A1.

Same research area

Search Inflammation/Immunology