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MEN2501 is an orally bioavailable small molecule inhibitor of the mitotic kinesin KIF18A, currently being developed by Stemline Therapeutics (a subsidiary of the Menarini Group). It is designed to selectively target cancer cells characterized by chromosomal instability (CIN+), a state frequently observed in advanced solid tumors such as platinum-resistant ovarian cancer. KIF18A is essential for chromosome alignment during mitosis in cells with chromosomal instability; by inhibiting its activity, MEN2501 triggers the spindle assembly checkpoint, leading to prolonged mitotic arrest and apoptosis. This targeted approach aims to exploit the specific mitotic vulnerabilities of aneuploid cancer cells while potentially minimizing toxicity to normal, chromosomally stable tissues.
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