AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC 50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
In Vivo
Tumor growth inhibition is statistically significant with AHR antagonist 5 as single. AHR antagonist 5 (10 mg/kg; p.o.; every day for 3 weeks) combination with anti-PD-1 significantly inhibited tumor growth inhibition compared to the anti-PD-1 alone . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Balb/c Mice (Mouse Colorectal Cancer Model CT26) Dosage: 10 mg/kg (combination with anti-PD-1) Administration: P.o.; every day for 3 weeks Result: Significantly inhibited tumor growth inhibition.