GSK461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM.
Cat.No
DC8598
Name
PLK1 inhibitor GSK461364
Chemical Properties
CAS
929095-18-1
Formula
C27H28F3N5O2S
MW
543.6
Storage
2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
References
[1]. Olmos D, 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.
[2]. Degenhardt Y, et al. Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability. Mol Cancer Ther. 2010 Jul;9(7):2079-89
[3]. Gilmartin AG, et al. Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis. Cancer Res. 2009 Sep 1;69(17):6969-77.
[4]. Chou YS, et al. Cytotoxic mechanism of PLK1 inhibitor GSK461364 against osteosarcoma: Mitotic arrest, apoptosis, cellular senescence, and synergistic effect with paclitaxel. Int J Oncol. 2016 Mar;48(3):1187-94.
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