Medchemexpress LLC TAK-960 dihydrochloride | 1137868-52-0 | C27H36Cl2F3N7O3 | 50 MG

Supplier:  Medchemexpress LLC HY15160B50MG

TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. It also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. This compound inhibits the proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.

• Causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3).
• Inhibits proliferation of multiple cancer cell lines (e.g., HT-29, HCT116, HeLa) with mean EC50 values from 8.4 to 46.9 nM, not affecting normal cells.
• In HeLa cells, 8 nM leads to G2/M cell cycle arrest without significant cytotoxicity.
• In animal models, it shows substantial antitumor activity and good tolerability against HT-29 colorectal cancer xenografts.

Catalog No. 50-003-72165