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GSK461364 is a potent, selective, and reversible small molecule inhibitor of Polo-like kinase 1 (Plk1), a serine/threonine protein kinase involved in regulating mitotic spindle function and cell cycle progression. It acts as an ATP-competitive inhibitor with high selectivity for Plk1 over other kinases. GSK461364 induces G2/M cell cycle arrest followed by apoptosis in tumor cells while causing reversible cell cycle arrest without apoptosis in normal cells. The drug has demonstrated cytostatic and cytotoxic effects across various cancer cell lines and shows efficacy in xenograft tumor models. Developed by GSK for the treatment of solid tumors and non-Hodgkin's lymphoma, its maximum clinical trial phase reached Phase I.
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