TAK-960 is a n orally available PLK1 inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor TAK-960 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressed tumor cells. PLK1, named after the polo gene of Drosophila melanogaster, is a serine/threonine kinase crucial in the regulation of mitosis.
CAS Number: 1137868-52-0
Molecular Weight: 561.60
Chemical Name: 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
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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. TAK-960 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells.
TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. 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.
- Talati C, Griffiths EA, Wetzler M, Wang ES. Polo-like kinase inhibitors in hematologic malignancies. Crit Rev Oncol Hematol. 2016 Feb;98:200-10. doi: 10.1016/j.critrevonc.2015.10.013. Epub 2015 Nov 4. PMID: 26597019.
- Inoue M, Yoshimura M, Kobayashi M, Morinibu A, Itasaka S, Hiraoka M, Harada H. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666. doi: 10.1038/srep15666. PMID: 26503893; PMCID: PMC4621528.
- Nair JS, Schwartz GK. Inhibition of polo like kinase 1 in sarcomas induces apoptosis that is dependent on Mcl-1 suppression. Cell Cycle. 2015;14(19):3101-11. doi: 10.1080/15384101.2015.1078033. PMID: 26236920; PMCID: PMC4825583.
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