tcsc3412 Mps1-IN-3

Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC₅₀ of 50 nM.

IC50 & Target: IC50: 50 nM (MPS1)^[1]

In Vitro: Mps1-IN-3 is a potent MPS1 kinase inhibitor, with an IC₅₀ of 50 nM. Mps1-IN-3 inhibits the proliferation of U251 glioblastoma cells with an IC₅₀ of appr 5 µM. Mps1-IN-3 (2 μM) can completely abrogates checkpoint. Furthermore, Mps1-IN-3 (5 μM) sensitizes all glioblastoma cells (U251, U87, VU147 and GBM8) to 3 nM of vincristine^[1].

In Vivo: Mps1-IN-3 (2 mg/kg, i.v.) sensitizes glioblastoma cells to vincristine in murine tumor models, with prolonged survival and no toxicity^[1].