Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

AHR (U87 cells):39.9 μM, CYP1A1 (U937 cells):70.7 μM, AhR (human cells):39.9 nM

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. [1]
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. [1]

METHODS: Bindarit (AF2838)(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. [1]