RP-1664 is a selective and orally active inhibitor of Polo-like kinase 4 (PLK4) with an IC50 of 3 nM. This compound exhibits remarkable selectivity toward PLK4 compared to related kinases such as AURKA, AURKB, and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells, resulting in the accumulation of PLK4 and p21 proteins. Its anti-tumor activity has been demonstrated in models of breast cancer and neuroblastoma, particularly in TRIM37-high-expressing cellular contexts.
RP-1664 is a selective and orally active inhibitor of Polo-like kinase 4 (PLK4) with an IC50 of 3 nM. This compound exhibits remarkable selectivity toward PLK4 compared to related kinases such as AURKA, AURKB, and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells, resulting in the accumulation of PLK4 and p21 proteins. Its anti-tumor activity has been demonstrated in models of breast cancer and neuroblastoma, particularly in TRIM37-high-expressing cellular contexts.
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