BAY-218

SKU: orb1301645

Description

BAY-218

Research Area

Immunology & Inflammation, Metabolism Research

Key Properties

• CAS Number: 2162982-11-6
• MW: 401.82
• Purity: 99.95% (May vary between batches)
• Formula: C₂₀H₁₇ClFN₃O₃
• SMILES: C[C@@H](CO)NC(=O)c1cc(nn(-c2cccc(F)c2)c1=O)-c1ccc(Cl)cc1
• Target: Aryl Hydrocarbon Receptor,AhR
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (8.21 mM);DMSO:252 mg/mL (627.15 mM)

Bioactivity

• Target IC50:
  CYP1A1 (U937 cells):70.7 μM|AhR (human cells):39.9 nM|AHR (U87 cells):39.9 μM
• In Vivo:
  METHODS: BAY-218 (30 mg/kg, oral, twice daily) and aPD-L1 (10 mg/kg, intraperitoneal injection, twice daily) were used to treat mice with CT26 tumor cell xenografts injected subcutaneously in the flank to observe their anti-tumor ability. RESULTS Combination therapy of BAY-218 and aPD-L1 inhibited tumor growth in mice.
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• In Vitro:
  METHODS: Human monocytic U937 cells were treated with BAY-218 (AHR antagonist 1)(1 nM, 3nM, 10nM, 30nM, 100nM, 300nM, 1 μΜ and 3μΜ) and the IC50 values were determined. RESULTS BAY-218 exhibited CYP1A1 inhibitory activity with an IC50 of 70.7 μM in the human monocytic U937 cell line. METHODS: BAY-218 (72 pM, 0.25 nM, 0.89 nM; 3.1 nM, 1 1 nM, 38 nM, 130 nM, 470 nM, 1.6 pM, 5.7 p, 20 μM) was used to treat U87 glioblastoma cells endogenously expressing AHR and the IC50 value was determined. RESULTS BAY-218 could inhibit the activity of AHR in U87 glioblastoma cells with an IC50 of 39.9 μM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ArylHydrocarbonReceptor, aryl hydrocarbon receptor (AHR), Aryl Hydrocarbon Receptor, BAY 218, BAY218, BAY-218, cancer, AHR antagonist 1, AHR antagonist1, AHR antagonist-1, AhR, inhibit, immune, Inhibitor, human monocytic U937 cells, U87 glioblastoma cells

Compound Identifiers

PubChem CID

132168144