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GSK461364

Chemical Structure : GSK461364

CAS No.: 929095-18-1

GSK461364 (GSK461364A, GSK-461364)

Catalog No.: PC-45884Not For Human Use, Lab Use Only.

GSK461364 is a potent, selective, and reversible ATP-competitive PLK1 inhibitor with Ki of 2.2 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK461364 is a potent, selective, and reversible ATP-competitive PLK1 inhibitor with Ki of 2.2 nM.
GSK461364 displays >390-fold greater selectivity for Plk1 than for Plk2 and Plk3 and 1,000-fold greater selectivity than for a panel of 48 other kinases.
GSK461364 shows antiproliferative activity against >120 tumor cell lines and potently inhibits the proliferation with IC50s of <100 nM.
GSK461364 shows clear antitumor activity in human tumor xenograft models.

Physicochemical Properties

M.Wt 543.6038
Formula C27H28F3N5O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Thiophenecarboxamide, 5-[6-[(4-methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-

References

1. Olmos D, et al. Clin Cancer Res. 2011 May 15;17(10):3420-30.

2. Gilmartin AG, et al. Cancer Res. 2009 Sep 1;69(17):6969-77.

3. Degenhardt Y, et al. Mol Cancer Ther. 2010 Jul;9(7):2079-89.

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