TAK-960 Inhibitor

TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2nM for Plk1, Plk2, and Plk3, respectively.

1. Klauck P J, Bagby S M, Capasso A, et al. Antitumor activity of the polo-like kinase inhibitor, TAK-960, against preclinical models of colorectal cancer[J]. BMC Cancer, 2018, 18 (1):136.
2. Hikichi Y, Honda K, Hikami K,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[J].Mol Cancer Ther. 2012 Mar;11 (3):700-9.
3. Nie Z, Feher V, Natala S, et al. Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1).[J]. Bioorganic & Medicinal Chemistry Letters, 2013, 23 (12):3662-3666.
4. 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.

Small volumes of TAK-960, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5752404 is an inhibitor targeting TAK-960.