In Vitro: IDO1-IN-2 inhibits amino-cyclobutarene-derived indoleamine-2,3-dioxygenase 1 (IDO1) Hela cellular with an IC50 of 49 nM. IDO1-IN-2 has an IC50 of 249 nM for IDO1 wholr blood.
In Vivo: IDO1-IN-2 (100 mg/kg, twice daily) demonstrates good efficacy synergy when combined with anti-PD-1 mAb in a mouse EMT6 tumor syngeneic model. IDO1-IN-2 has a t1/2 of 3.7 hours, a CL/CLu of 15/319 mL/min/kg, and a F of 63% for rats. IDO1-IN-2 has a t1/2 of 6 hours, a CL/CLu of 6/88 mL/min/kg, and a F of 67% for dogs.