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No.BCP0007 
Product Name:GSK461364 
Cas No.:929095-18-1 

M.Wt: 543.6

Formula: C27H28F3N5O2S

Solubility: Unknown

Purity: >99%

Storage: -20℃ 2 years

10g in stock

 

GSK461364, a selective i.v. thiophene amide inhibitor of PLK1, induced selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. GSK461364 is an ATP-competitive inhibitor of Plk1 and forms a rapidly reversible complex with Plk1. It has a 400-fold greater potency for Plk1 than for Plk2 and Plk3.In vitro, this compound showed antiproliferative activity in ??120 cancer cell lines tested. IC50 values were ??50 nM in ??83% of the cell lines tested. GSK461364 demonstrated tumor growth inhibition in animal models. In these xenograft models, GSK461364 showed antitumor activity ranging from complete tumor growth inhibition to growth delay. Interestingly, the compound caused dose-dependent mitotic arrest in Colo205 xenografts in vivo.

1. Sch ffski P. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009 Jun;14(6):559-70. Epub 2009 May 27.

2. Laquerre S, Sung C-M, Gilmartin A et al. A potent and selective Polo-like kinase 1 (Plk1) inhibitor (GSK461364) induces cell cycle arrest and growth inhibition of cancer cell. Presented at the 98th American Association for Cancer Research Annual Meeting, Los Angeles, CA, April 14?C18, 2007.

3. Erskine S, Madden L, Hassler D et al. Biochemical characterization of GSK461364: A novel, potent, and selective inhibitor of Polo-like kinase-1 (Plk1). Presented at the 98th American Association for Cancer Research Annual Meeting, Los Angeles, CA, April 14?C18 2007.

4. Sutton D, Diamond M, Faucette L et al. Efficacy of GSK461364, a selective Plk1 inhibitor, in human tumor xenograft models. Presented at the 98th American Association for Cancer Research Annual Meeting, Los Angeles, CA, April 14?C18, 2007.

 

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