TAK-960

TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts[1].

Product Specifications

CAS Number

[1137868-52-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TAK-960.html

Purity

99.75

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C=C2F

Molecular Formula

C27H34F3N7O3

Molecular Weight

561.60

Precautions

H302, H315, H319, H335

References & Citations

[1]Hikichi Y, et al. 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 Mar;11 (3) :700-9.|[2]Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.