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

TAK-960 treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 (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 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells^[2].

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

561.60

Solid

C₂₇H₃₄F₃N₇O₃

1137868-52-0

Room temperature in continental US; may vary elsewhere.

DMSO : 16.67 mg/mL(29.68 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。