产品描述:
MLN0905 is an inhibitor of polo-like kinase 1 (Plk1; IC50 = 2 nM).{20484} It inhibits 95% of Plk1 activity but also inhibits the activity of 10 additional kinases by greater than or equal to 90% in a panel of 359 kinases at 1 µM. MLN0905 reduces phosphorylation of histone H3 at serine 10 (H3S10Ph), a marker of cell cycle arrest at prometaphase, in HT-29 colorectal cancer cells (EC30 = 9 nM). It inhibits proliferation in a panel of six human lymphoma cell lines with IC50 values ranging from 3.2 to 24 nM.{57365} MLN0905, alone or in combination with rituximab, increases survival in an OCI LY-19 metastatic lymphoma mouse xenograft model.