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Submit ReviewTAK 960 hydrochloride
Description: Potent and selective PLK1 inhibitor
Chemical Name: 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 hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for TAK 960 hydrochloride
TAK 960 hydrochloride is a potent PLK1 inhibitor (IC50 values are 0.8, 16.9 and 50.2 nM for PLK1, PLK2 and PLK3 respectively). Exhibits >20-fold selectivity for PLK1 over FAK, MLCK and FES, and has minimal activity against a panel of 282 other kinases. Inhibits proliferation of a range of cancer cell lines in vitro and inhibits tumor growth of multiple human cancer cell xenografts in vivo. Orally bioavailable.
Compound Libraries for TAK 960 hydrochloride
TAK 960 hydrochloride is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for TAK 960 hydrochloride
| M. Wt | 598.06 |
| Formula | C27H34F3N7O3.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2108449-45-0 |
| PubChem ID | 91826087 |
| InChI Key | QZBHDFGFNVMONB-UHFFFAOYSA-N |
| Smiles | O=C1C(F)(F)CN(C3CCCC3)C(N=C(NC4=CC(F)=C(C(NC5CCN(C)CC5)=O)C=C4OC)N=C2)=C2N1C.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TAK 960 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 59.81 | 100 |
Preparing Stock Solutions for TAK 960 hydrochloride
The following data is based on the product molecular weight 598.06. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.67 mL | 8.36 mL | 16.72 mL |
| 5 mM | 0.33 mL | 1.67 mL | 3.34 mL |
| 10 mM | 0.17 mL | 0.84 mL | 1.67 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
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Product Datasheets for TAK 960 hydrochloride
References for TAK 960 hydrochloride
References are publications that support the biological activity of the product.
Hikichi et al (2012) 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. 11 700 PMID: 22188812
Nie et al (2013) Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Bioorg.Med.Chem.Lett. 23 3662 PMID: 23664874
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Keywords: TAK 960 hydrochloride, TAK 960 hydrochloride supplier, TAK960, hydrochloride, potent, PLK1, inhibitors, inhibits, selective, orally, bioavailable, antitumor, 1137868520, Polo-like, Kinase, Mitosis, 5403, Tocris Bioscience
1 Citation for TAK 960 hydrochloride
Citations are publications that use Tocris products. Selected citations for TAK 960 hydrochloride include:
Marc R et al (2023) Predicting anti-cancer drug combination responses with a temporal cell state network model. PLoS Comput Biol 19 e1011082 PMID: 37126527
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.