RO0505124

RO0505124 is a selective CDK4 inhibitor with an IC₅₀ of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitosis, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer^[1]. In Vitro:RO0505124 (30 min) potently and selectively inhibits recombinant human CDK4-cyclin D with an IC₅₀ of 20 nM, showing >100-fold selectivity over CDK1 and CDK2, and relatively high selectivity across a panel of 128 kinases^[1].
RO0505124 (48 h) inhibits proliferation of multiple human cancer cell lines with IC₅₀ values ranging from 1.45 μM to 8.12 μM after 48 h of treatment^[1].
RO0505124 (3.9-18.3 μM; 4-24 h) induces a G₁ phase arrest and inhibits Rb phosphorylation in asynchronous HCT-116 cells^[1].
RO0505124 (2 μM; 0-24 h) delays mitotic entry, prolongs mitotic duration, and induces aberrant mitosis^[1].
RO0505124 (2 μM; 3-14 h) delays the accumulation of survivin and borealin proteins during G₂/M phase in HeLa cells^[1].