IC50: 8.4 to 46.9 nmol/L for multiple cancer cell lines
Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase involved in key mitosis processes. Human PLK1 has been shown to be overexpressed in various human cancers. Elevated levels of PLK1 have been associated with poor prognosis, making it an attractive target for anticancer therapy. TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor.
In vitro: TAK-960 treatment caused accumulation of G2–M cells, aberrant polo mitosis morphology, and increased the phosphorylation of histone H3. TAK-960 inhibited proliferation of multiple cancer cell lines, with mean EC50 ranging from 8.4 to 46.9 nmol/L, but not in nondividing normal cells .
In vivo: In animal models, oral administration of TAK-960 increased pHH3 in a dose-dependent manner and significantly inhibited the growth of HT-29 colorectal cancer xenografts. Once daily treatment TAK-960 exhibited significant efficacy against multiple tumor xenografts, including an adriamycin/paclitaxel-resistant xenograft model and a disseminated leukemia model .
Clinical trial: TAK-960 is currently undergoing Phase I evaluation in adult patients with advanced non-hematologic malignancies.
 Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E. 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.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥28.05mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|