TAK-960 (TAK960) is a novel, investigational, orally bioavailable, and selective inhibitor of polo-like kinase 1 (PLK1) with anticancer activity. TAK-960 also exhibits inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. It inhibits PLK1 with an IC50 of 0.8 nM at 10 μM ATP.Serine/threonine protein kinase PLK1 is essential for several processes in mitosis. Human PLK1 is a promising target for anticancer therapy because it has been demonstrated to be overexpressed in a variety of human cancers and because elevated levels of PLK1 have been linked to a poor prognosis. Multiple tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1), have demonstrated TAK-960's efficacy. TAK-960 treatment resulted in G(2)-M cell accumulation, abnormal polo mitosis morphology, and elevated phosphorylation of histone H3 (pHH3) in vitro and in vivo, all of which were consistent with PLK1 inhibition. TAK-960 did not affect nondividing normal cells (EC(50) >1,000 nmol/L), but it did inhibit the proliferation of several cancer cell lines, with mean EC(50) values ranging from 8.4 to 46.9 nmol/L. In the tested cell lines, there was no correlation found between the potency of TAK-960 and the mutation status of TP53, KRAS, and MDR1 expression. Oral administration of TAK-960 in animal models resulted in a dose-dependent increase in pHH3 and a significant inhibition of the growth of HT-29 colorectal cancer xenografts. The administration of TAK-960 once daily demonstrated noteworthy effectiveness against various tumor xenograft models, such as a disseminated leukemia model and an adriamycin/paclitaxel-resistant xenograft model. TAK-960 is currently being evaluated clinically in patients with metastatic cancer.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.