CZL-S092 is a PLK4 inhibitor with exceptional selectivity for other PLK4 family members (PLK1, PLK2, and PLK3), exhibiting an IC50 of 0.9 nM. It demonstrates antineuroblastoma activity in vitro (IMR-32, IC50 = 1.143 μM) and shows good oral bioavailability in vivo (SD rats, F = 22.1%). CZL-S092 is applicable in research on various cancers, including neuroblastoma.

CZL-S092 (Compound 34b) at a concentration of 0.5 μM for 60 minutes demonstrates significant inhibitory activity against PLK4 among 37 tested kinases, with an inhibition rate greater than 80%, and exhibits high selectivity for other PLK family members (PLK1, PLK2, and PLK3). At concentrations ranging from 0.5 to 2.5 μM over 5 days, CZL-S092 shows notable antiproliferative effects on MCF-7, IMR-32, and SH-SY5Y cells, with IC50 values of 2.828 μM, 1.143 μM, and 1.329 μM, respectively. At concentrations of 1.0 to 5.0 μM for 48 hours, CZL-S092 significantly induces apoptosis in IMR-32 cells (84.3%) and causes cell cycle arrest at the G2/M phase (87.4%). Additionally, at 1.0 to 5.0 μM for 24 hours, CZL-S092 markedly inhibits the migration of IMR-32 cells (over 90%).