MLN0905

MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC₅₀ value of 2 nM. MLN0905 can be used for the research of cancer^[1][2]. IC50 & Target:IC50: 2 nM (PLK1); EC50: 33 nM (Cdc25C); LD50: 22 nM (HT29 cells), 56 nM (HCT116 cells), 89 nM (H460 cells) and 34 nM (A375 cells)^[1].
IC50: 3 - 24 nM (lymphoma cell lines)^[2]. In Vitro:MLN0905 (compound 12c) has inhibitory potency against PLK1 with an IC₅₀ value of 2 nM^[1].
MLN0905 exhibits potent activities for Cdc25C with an EC₅₀ value of 33 nM^[1].
MLN0905 shows inhibitory effects on HT29, HCT116, H460, and A375 cell lines with LD₅₀ values of 22 nM, 56 nM, 89 nM and 34 nM, respectively^[1].
MLN0905 (125 nM) shows strong mitotic arrest and monopolar spindle formation in HT-29 cells^[1].
MLN0905 suppresses the growth of lymphoma cell lines with IC₅₀ values ranging from 3 - 24 nM^[2]. In Vivo:MLN0905 (p.o.; 50 mg/kg) shows a high sustained PD response in nude mice HT29 xenograft tumors^[1].
MLN0905 (p.o.; 6.25, 12.5, 25, 50 mg/kg) exhibits significant antitumor activities in mice HT29 xenograft tumors^[1].
MLN0905 (p.o.; 0-14.5 mg/kg; daily, QD×3/week) has marked antitumor effects in kinds of lymphoma xenograft model^[1][2].