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CCT271850 is a potent, selective, and orally bioavailable small molecule inhibitor of monopolar spindle 1 (Mps1) kinase (also known as TTK protein kinase), with an IC50 of 0.004 μM. Developed by the Institute of Cancer Research (ICR), London, CCT271850 targets the spindle assembly checkpoint (SAC) during mitosis. By inhibiting Mps1, it prevents proper chromosome alignment and causes premature mitotic exit, leading to severe chromosome missegregation, aneuploidy, and apoptotic cell death. Preclinical studies have demonstrated its efficacy as a single agent or in combination with taxanes in various human cancer models, particularly in PTEN-deficient breast cancer and colorectal cancer.
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