TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner (IC50: 0.84 μM). TC-Mps1-12 inhibits the growth of pMps1 cell lines (IC50: 131 nM in autophosphorylation assay) [1].

TC-Mps1-12 (25-100 mg/kg; p.o.; daily; for 19 days) inhibits the growth of A549 cells in a dose-dependent manner in vivo. TC-Mps1-12 (100 mg/kg) treatment shows 47% tumor growth inhibition without body weight loss. TC-Mps1-12 (p.o., 25 mg/kg)treatment displays good PK properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL [1].