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

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

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

634.52

Solid

C₂₇H₃₆Cl₂F₃N₇O₃

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

H₂O : 10 mg/mL(15.76 mM;Need ultrasonic)

DMSO : 3.23 mg/mL(5.09 mM;Need ultrasonic)

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 (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。