TAK 960 hydrochloride

Name: TAK 960 hydrochloride
Brand: Tocris Bioscience
SKU: 5403

Tocris Bioscience, part of Bio-Techne | Catalog # 5403

Citations (2)

COA / SDS

Potent and selective PLK1 inhibitor

Key Product Details

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)
Molecular Weight:	598.06

View Full Technical Details for TAK 960 hydrochloride

Technical Data
Citations

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 for TAK 960 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for TAK 960 hydrochloride

References are publications that support the biological activity of the product.

Nie Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Bioorg.Med.Chem.Lett. 2013 PMID: 23664874
Hikichi 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 PMID: 22188812