TAK-960 MedChemExpress (MCE)

Product Name	TAK-960
Synonyms	CS-554 TAK960 TAK-960 TAK 960 CS-1725 4-((9-Cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide Synonyms CS-554 TAK960 TAK-960 TAK 960 CS-1725 4-((9-Cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide 4-[(9-Cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)benzamide Benzamide, 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)-
CAS	1137868-52-0
EINECS
Chemical Formula	C27H34F3N7O3
Molecular Weight	561.6
inchi
Package	10 mM * 1 mL;1 mg;2 mg;5 mg;10 mg;25 mg;50 mg
Price	Get quote
Descriptions	TAK-960 TAK-960 MedChemExpress (MCE) HY-15160 1137868-52-0 99.75% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions TAK-960 TAK-960 MedChemExpress (MCE) HY-15160 1137868-52-0 99.75% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts. 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 EC50 values 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]. PLK1 0.8 nM (IC50) PLK2 16.9 nM (IC50) PLK3 50.2 nM (IC50) FAK/PTK2 19.6 nM (IC50) MLCK/MYLK 25.6 nM (IC50) FES/FPS 58.2 nM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Hikichi Y, et al. TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar 11(3):700-9. [Content Brief] [2]. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27 5:15666. [Content Brief]
Last Update	2025-04-01 14:45:47

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