TAK-960 monohydrochloride is an orally available, selective inhibitor ofpolo-like kinase1 (PLK1), with anIC₅₀of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities againstPLK2andPLK3, with IC₅₀s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiplecancercell lines and exhibits significant efficacy against multiple tumor xenografts^[1].

TAK-960 monohydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 monohydrochloride (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC₅₀values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells^[1].
TAK-960 monohydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells^[2].

TAK-960 monohydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts^[1].
In animal models, TAK-960 monohydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts^[1].

598.06

C₂₇H₃₅ClF₃N₇O₃

2108449-45-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.