IV-361, an orally active and selective CDK7 inhibitor with a Ki value of less than or equal to 50 nM, demonstrates potent anti-cancer activity (US20190256531A1).

CDK2:≥1000 nM (Ki), CDK7:≤50 nM (Ki)

IV-361 demonstrates minimal inhibitory effects on CDK2 (K i ≥1000 nM) and PLK1 (K i ≥5000 nM), highlighting its specificity[1]. Moreover, it exhibits potent inhibition of IL-2 and IL-17 production (all IC 50 ≤100 nM) in peripheral blood mononuclear cells (PBMC), alongside significant growth inhibitory activity against HCT-116 cells (GI 50 ≤100 nM)[1].

IV-361, administered orally at a dosage of 25 mg/kg/day, demonstrates a suppression rate of 46% or greater in tumor volume in female BALB/c nude mice implanted with HCT-116[1].