GSK461364

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM). It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases. GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis. It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier. GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.Formal Name: 5-[6-[(4-methyl-1-piperazinyl)methyl]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide. CAS Number: 929095-18-1. Synonyms: GSK461364A. Molecular Formula: C27H28F3N5O2S. Formula Weight: 543.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 272, 307 nm. SMILES: CN1CCN(CC1)CC2=CC3=C(C=C2)N=CN3C4=CC(O[C@H](C)C5=C(C(F)(F)F)C=CC=C5)=C(S4)C(N)=O. InChi Code: InChI=1S/C27H28F3N5O2S/c1-17(19-5-3-4-6-20(19)27(28,29)30)37-23-14-24(38-25(23)26(31)36)35-16-32-21-8-7-18(13-22(21)35)15-34-11-9-33(2)10-12-34/h3-8,13-14,16-17H,9-12,15H2,1-2H3,(H2,31,36)/t17-/m1/s1. InChi Key: ZHJGWYRLJUCMRT-QGZVFWFLSA-N.