533380 Sigma-AldrichPolo-like Kinase Inhibitor VI, NMS-P937 - CAS 1034616-18-6 - Calbiochem

This product has been discontinued.

A cell-permeable, orally bioavailable, dihydropyrazoloquinazoline based compound that acts as a highly potent, reversible, and ATP-competitive inhibitor of polo-like kinase 1 (Plk1; IC₅₀ = 2 nM). Displays excellent selectivity over Plk2 and Plk3 (IC₅₀ > 10 µM). At higher concentrations affect the activities of fms-like tyrosine kinase (Flt3), maternal embryonic leucine zipper kinase (MELK), and casein kinase 2 (IC₅₀ = 510, 744 and 826 nM, respectively). Preferentially blocks cell cycle at G2/M phase and induces apoptosis in cancer cells (IC₅₀ = 42 nM in A2780 human ovarian carcinoma cells). Shown to suppress the growth of HCT116 colon adenocarcinoma cells xenografted in CD1 nu/nu mice (45 mg/kg, b.i.d). Also exhibits good potency on taxol (Cat. No. 580555) resistant tumor cells (IC₅₀ = 65 and 62 nM for A2780 and 1A9 PTX ovarian adenocarcinoma cells, respectively). Displays desirable pharmacokinetic properties with t_1/2 = 0.9 h; AUC = 8.7 µM/h; clearance = 2.36 L/h/kg (10 mg/kg, i.v.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.