Mps1-IN-5 is a potent, orally active Mps1 inhibitor exhibiting an IC50 of 29 nM, known for triggering apoptosis and G2/M phase cell cycle arrest. This compound demonstrates antiproliferative and anti-tumor effects by inhibiting Mps1 phosphorylation and inducing DNA damage [1].

Mps1-IN-5 (compound 12) inhibited the proliferation of MCF-7 and 4T1 cells in a time-dependent manner at 0-10 µM over 24, 48, and 72 hours [1]. It induced apoptosis and caused G2/M phase cell cycle arrest in a dose-dependent manner at 0, 0.5, 1.0, and 5.0 µM for 24 and 48 hours [1]. Additionally, at 0, 0.03, 0.1, 1, or 3 µM for 2 hours, the compound inhibited Mps1 phosphorylation and induced DNA damage [1].

Mps1-IN-5 (30, 60 mg/kg; oral administration; daily for 15 days) effectively suppresses tumor growth in a breast cancer model without significant toxicity [1].