For research use only. Not for therapeutic Use.
TAK-960（Cat No.:I000520）is a selective inhibitor of polo-like kinase 1 (PLK1), an essential regulator of cell division. By inhibiting PLK1, TAK-960 disrupts key processes during mitosis, such as spindle formation and chromosome segregation, leading to cell cycle arrest and apoptosis in cancer cells. Its potent anti-proliferative effects make TAK-960 a promising candidate for treating various cancers, particularly those characterized by uncontrolled cell division. Preclinical studies have shown its potential in treating colorectal cancer and other solid tumors, highlighting its role in targeted cancer therapies focused on mitotic regulation.
| Catalog Number | I000520 |
| CAS Number | 1137868-52-0 |
| Synonyms | 4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide |
| Purity | ≥95% |
| Target | Polo-like Kinase (PLK) |
| Solubility | DMSO: ≥ 35 mg/mL |
| Storage | Store at -20°C |
| IC50 | 1.5 nM |
| Reference | </br>1:Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1). Nie Z, Feher V, Natala S, McBride C, Kiryanov A, Jones B, Lam B, Liu Y, Kaldor S, Stafford J, Hikami K, Uchiyama N, Kawamoto T, Hikichi Y, Matsumoto S, Amano N, Zhang L, Hosfield D, Skene R, Zou H, Cao X, Ichikawa T.Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6. doi: 10.1016/j.bmcl.2013.02.083. Epub 2013 Feb 27. PMID: 23664874 </br>2:TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. 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.Mol Cancer Ther. 2012 Mar;11(3):700-9. doi: 10.1158/1535-7163.MCT-11-0762. Epub 2011 Dec 21. PMID: 22188812 Free Article |
