CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 ( PLK4 ) ( IC50 =2.6 nM). CZS-241 hydrochloride inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 hydrochloride induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 hydrochloride shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines [1].
References:
[1]. Sun Y, et al. Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia. J Med Chem. 2023 Feb 23;66(4):2396-2421.
References:
[1]. Sun Y, et al. Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia. J Med Chem. 2023 Feb 23;66(4):2396-2421.