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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.
| Cas No. | 929095-18-1 |
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| Purity | ≥99% |
| 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 |
| Solubility | Ethanol 30 mg/mL (55.18 mM) DMSO 10 mg/mL (18.39 mM) Water Insoluble |
| Appearance | White to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
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.