GSK-461364
GSK-461364 is an inhibitor of polo-like kinase 1 (PLK1) that is currently in clinical trials as a potential treatment for solid tumor cancers. GSK-461364 displays anticancer chemotherapeutic activity as well as anticoagulant activity. This compound inhibits glioblastoma cell proliferation, invasion, and colony formation and induces apoptosis and G2 phase cell cycle arrest.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18929646
| Cas No. |
929095-18-1 |
|---|---|
| Purity |
≥98% |
| Formula |
C27H28F3N5O2S |
| Formula Wt. |
543.60 |
| IUPAC Name |
5-{6-[(4-Methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl}-3-{(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy}-2-thiophenecarboxamide |
| Appearance |
White to off white powder |
Yim H. Current clinical trials with polo-like kinase 1 inhibitors in solid tumors. Anticancer Drugs. 2013 Nov;24(10):999-1006. PMID: 23949254.
Pezuk JA, Brassesco MS, Morales AG, et al. Polo-like kinase 1 inhibition causes decreased proliferation by cell cycle arrest, leading to cell death in glioblastoma. Cancer Gene Ther. 2013 Sep;20(9):499-506. PMID: 23887645.
Olmos D, Barker D, Sharma R, et al. Phase I study of GSK461364, a specific and competitive Polo-like kinase 1 inhibitor, in patients with advanced solid malignancies. Clin Cancer Res. 2011 May 15;17(10):3420-30. PMID: 21459796.
