TAK 960 hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 5403 - TAK 960 hydrochloride | C27H34F3N7O3.HCl | CAS No. 1137868-96-2
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
Literature

Biological Activity

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

TAK 960 hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 598.06
Formula C27H34F3N7O3.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1137868-96-2
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 59.81 100

Preparing Stock Solutions

The following data is based on the product molecular weight 598.06. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair

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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.

Pathways for TAK 960 hydrochloride

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