CZS-241

CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM) . CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines[1].

Product Specifications

CAS Number

[3016297-55-2]

UNSPSC

12352005

Target

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

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/czs-241.html

Solubility

10 mM in DMSO

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

Molecular Formula

C26H24ClF2N9O

Molecular Weight

551.98

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.