IDO1-IN-7, a potent and selective indoleamine-2,3-dioxygenase-1 (IDO1) inhibitor, exhibits high potency with an IC 50 of 6.1 nM in the cellular assay (SKOV3). Apart from its inhibitory properties, IDO1-IN-7 also demonstrates immunomodulatory effects, contributing to its potential applications in cancer research.

IDO1 (SKOV3 cells):6.1 nM (IC50)

IDO1-IN-7 demonstrates moderate effectiveness in inhibiting target activity in a human whole blood assay, achieving an IC50 of 330 nM[1]. It also exhibits a favorable profile, characterized by good metabolic stability and satisfactory off-target selectivity[1]. Moreover, IDO1-IN-7 displays high specificity for IDO1, significantly outperforming tryptophan 2,3-dioxygenase (TDO) with an IC50 of 14,000 nM, highlighting its selectivity[1].

IDO1-IN-7, administered orally at a dosage of 10 mg/kg, demonstrates a maximal concentration (C max) of 10.0 μM and an area under the curve (AUC) from 0 to 8 hours of 27.1 μM*h, with a half-life (t 1/2) of 1.4 hours in mice. [1] This pharmacokinetic analysis was conducted in a mouse model.