TAK-960 has shown activity in several tumor cell lines including those that express multi-drug resistant protein 1 (MDR1). Consistent with PLK1 inhibition, TAK-960 treatment gives rise to accumulation of G2/M cells, aberrant "polo" mitosis morphology, and increases phosphorylation of histone H3 (pHH3). TAK-960 inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM. TAK-960 is an inhibitor of Plk.
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Nair et alNair et al. (PubMed ID 26236920) found that the kinase 1 (PLK-1) inhibitor TAK-960 induced apoptosis in sarcoma cell lines via down-regulation of Mcl-1 and PLK1 by siRNA. -SCBT Publication Review
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