Synonyms: (R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide; 5-[6-[(4-Methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide; GSK461364
Molecular Formula: C27H28F3N5O2S
Molecular Weight: 543.6
Linear Structural Formula: C27H28F3N5O2S
MDL Number: MFCD12755419
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: GSK461364 is an imidazotriazine derivate that inhibits polo-like kinase 1 (Plk1) in a potent, reversible, ATP-competitive, and highly selective manner (Kiapp<0.5 nm vs. 0.86 mum for plk2 and 200 mum for plk3; atp kmapp="16" mum), exhibiting much reduced or little potency toward a panel of 262 kinases. gsk461364a inhibits the growth of various cancer cultures (ig50 <100 nm) as a result of either growth arrest (cytostasis) or cytotoxicity in vitro and effectively suppresses the expansion of various human tumor exnografts in mice in vivo (25 or 50 mg g i.p. q2dx12).<>