Debio 0123 (Debio0123) is a potent, orally available, and highly selective Wee1 kinase inhibitor with IC50 of 0.8 nM, Ki of 0.1 nM.
Debio 0123 is highly selective to Wee1 on 465 selected kinases in a cellfree system, does not inhibit Plk1 and Plk2, as also reported in recent publications for AZD1775.
Debio 0123 exhibits in vitro growth inhibition activity in a broad number of human cancer cell lines (IC50= 0.109 to 7.08 uM).
Debio 0123 prevent CDC2 / Cdk1 phosphorylation, induces γH2AX and enhances phosphorylation of histone H3.
Debio 0123 induces apoptosis through mitotic catastrophe following cell cycle progression despite accumulation of unrepaired DNA damage both in vitro and in vivo.
