TAK-960 | PLK1 inhibitor | Probechem Biochemicals

Chemical Structure : TAK-960

CAS No.: 1137868-52-0

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TAK-960 (TAK960)

货号: PC-25813Not For Human Use, Lab Use Only.

TAK-960 is a potent, selective, ATP-competitive, orally available inhibitor of polo-like kinase 1 (PLK1) with IC50 of 1.6 nM in TR-FRET assays.

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5 mg	￥980	In stock
10 mg	￥1480	In stock
25 mg	￥2580	In stock
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100 mg		Get quote

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生物&药学活性

TAK-960 is a potent, selective, ATP-competitive, orally available inhibitor of polo-like kinase 1 (PLK1) with IC50 of 1.6 nM in TR-FRET assays.
TAK-960 inhibits full-length PLK1 protein with IC50 of 0.8 nM, relatively inhibits PLK2 and PLK3 with IC50 of 16.9 and 50.2 nM, weakly inhibits FAK, MLCK, and FES kinases against a panel of 288 kinases.
TAK-960 (10-30 nM) induces accumulation of aberrant mitotic cells in HT-29 cells.
TAK-960 inhibits proliferation of human cancer cell lines regardless of TP53 and KRAS mutation and MDR1 expression status.
TAK-960 treatment caused accumulation of G2–M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3) in vitro and in vivo.
TAK-960 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.
TAK-960 significantly inhibited the growth of HT-29 colorectal cancer xenografts, exhibited significant efficacy against multiple tumor xenografts, including an adriamycin/paclitaxel-resistant xenograft model and a disseminated leukemia model.

物理化学性质&存储条件

分子量	561.61
分子式	C27H34F3N7O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Hikichi Y, et al. Mol Cancer Ther. 2012 Mar;11(3):700-9.

2. Nie Z, et al. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6.

TAK-960 (TAK960)

生物&药学活性

物理化学性质&存储条件

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TAK-960 (TAK960)

生物&药学活性

物理化学性质&存储条件

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