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 IC50& Target:PLK1 0.8 nM (IC 50 ) PLK2 16.9 nM (IC 50 ) PLK3 50.2 nM (IC 50 ) FAK/PTK2 19.6 nM (IC 50 ) MLCK/MYLK 25.6 nM (IC 50 ) FES/FPS 58.2 nM (IC 50 ) 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
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TAK-960 dihydrochloride
CAS number：unknown molecular formula：C27H36Cl2F3N7O3
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| Chinese alias | TAK-960 二盐酸盐 | ||
| English alias | - | ||
| CAS number | unknown | molecular formula | C27H36Cl2F3N7O3 |
| molecular weight | 634.52 g/mol | Exact mass | 10mM in Water |
| PSA | - | logp | - |
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