MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).

PLK1:2 nM

在携带HT-29异种移植物的裸鼠中,口服MLN0905（6.25 mg / Kg-50 mg / Kg）能够在治疗48小时后,表现剂量依赖的药效反应.在携带OCI LY-19-Luc肿瘤的小鼠中,口服MLN0905（3.12 mg / Kg-6.25 mg / Kg）在治疗后8小时表现药效反应.

MLN0905是PLK1抑制剂（IC50=2 nM）。 LN0905抑制细胞有丝分裂（EC50=9 nM）。在HT-29细胞中（LD50=22 nM）,MLN0905能够抑制细胞增殖。在一组淋巴瘤细胞中（IC50=3 - 24 nM）,MLN0905能够抑制细胞活力。

PLK1 Flash Plate Assay: The human PLK1 enzymatic reaction totaling 30μL contained 50 mM Tris-HCl (pH 8.0), 10 mM MgCl2, 0.02% BSA, 10% glycerol, 1 mM DTT, 100 mM NaCl, 3.3% DMSO, 8 μM ATP, 0.2μCi [γ- 33 P]-ATP, 4 μM peptide substrate (Biotin-AHX-LDETGHLDSSGLQEVHLA-CONH2), and 10 nM recombinant human PLK1[2–369]T210D. The enzymatic reaction mixture, with or without PLK inhibitors, is incubated for 2.5 h at 30℃before termination with 20μL of 150 mM EDTA. Then 25μL of the stopped enzyme reaction mixture is transferred to a 384-well streptavidin coated Image FlashPlate and incubated at room temperature for 3 h. The Image Flash Plate wells are washed three times with 0.02% Tween-20 and then read on the Perkin-Elmer Viewlux.