Orally bioavailable and highly selective small-molecule inhibitor of CDK4/6 (mean IC50 value 307 nM in sensitive neuroblastoma-derived cell lines). LEE011 caused cell-cycle arrest and cellular senescence that was attributed to dose-dependent decreases in phosphorylated RB and FOXM1, respectively. LEE 011 treatment of BE2C and IMR5 neuroblastoma cell lines with demonstrated sensitivity to CDK4/6 inhibition resulted in a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle.

KEYWORDS: LEE 011 | supplier | CDK4/6 inhibitor | Ribociclib | LEE011 | LEE-011 | CAS [1211441-98-3] | Cyclin Dependent | CDK4 | CDK6 | orally bioavailable | cell-cycle arrest | senescence | FOXM1