Mps1-IN-3 hydrochloride is a potent and selective Mps1 inhibitor with an IC50 value of 50 nM. Mps1-IN-3 hydrochloride can inhibit the proliferation of glioblastoma cells, and effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft model[1].
Mps1-IN-3 hydrochloride (0.3-10 μM) inhibits the marker of mitotic cells cyclin B in a dose-dependent manner[1].Mps1-IN-3 hydrochloride (2 μM) causes a dose-dependent escape from a checkpoint-mediated mitotic arrest[1]. Mps1-IN-3 hydrochloride (1-15 μM) inhibits the proliferation of U251 glioblastoma cells with an IC50 value of ~5 µM[1].
Mps1-IN-3 hydrochloride (2 mg/kg; IV, twice a week, for 3 weeks) effectively sensitizes glioblastomas to Vincristine in orthotopic glioblastoma xenograft models[1].
[1]. Tannous BA, et al. Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs. J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31.