CZS-241 is a potent, selective PLK4 inhibitor with IC50 of 2.6 nM for PLK4, >1000-fold selective over TRKA.
CZS-241 potently inhibits chronic myeloid leukemia (CML) cell lines K562 (IC50 =0.096 μM) and KU-812 (IC50 = 0.25 μM).
CZS-241 has high selectivity to other members of PLK family (PLK1-3), high homology kinases (Aurora B and TRK A/B).
CZS-241 exhibited promising in vivo efficacy in the chronic myeloid leukemia (CML) K562 cells xenograft mouse model.
