TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1) , with an IC 50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3 , with IC 50 s of 16.9 and 50.2 nM, respectively. TA
In Vitro:TAK-960 dihydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 dihydrochloride (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines,
In Vivo:TAK-960 dihydrochloride exhibits (10mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. In animal models, TAK-960 dihydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits th
Biological Activity:TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1) , with an IC 50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3 , with IC 50 s of 16.9 and 50.2 nM, respectively. TA