CZS-241 (hydrochloride)

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].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Polo-like Kinase (PLK) ; Trk Receptor

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Neuronal Signaling; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

FC1=CC=C(C=C1NC(C2=C(C=CC(CNC3=NC4=C(C(NC5=NNC(C)=C5)=N3)C=NN4C(C)C)=C2)Cl)=O)F.Cl

Molecular Formula

C26H25Cl2F2N9O

Molecular Weight

588.44

References & Citations

[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.