TAK 960 hydrochloride

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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)
Datasheet
Citations
Reviews
Literature (4)

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.

Select a batch to recalculate based on the batch molecular weight:
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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Citations for TAK 960 hydrochloride

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Literature in this Area

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