Description
InformationRoscovitine (CYC202, Seliciclib, R-roscovitine) is a potent and selective CDK inhibitor forCdc2,CDK2andCDK5withIC50of 0.65 µM, 0.7 µM and 0.16 µM in cell-free assays. It shows little effect on CDK4/6. Phase 2.In vitroRoscovitine displays high efficiency and high selectivity towards some cyclin-dependent kinases with IC50 of 0.65, 0.7, 0.7 and 0.16 µM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E and cdk5/p53, respectively. Roscovitine reversibly inhibits the prophaselmetaphase transition in the micromolar range of starfish oocytes and sea urchin embryos, inhibits in vitro M-phase-promoting factor activity and in vitro DNA synthesis in Xenopus egg extracts, and suppresses the proliferation of mammalian cell lines with an average IC50 of 16 µM. In mesangial cells, Roscovitine results in a dose-dependent reduction of CDK2 activity that at concentrations of 7.5, 12.5 and 25 mM, Roscovitine causes a 25, 50% and 100% decrease in CDK2 activity, respectively. A recent study shows that Roscovitine inhibits cdk5 kinase activity, cell proliferation, multicellular development, and cdk5 nuclear translocation in Dictyostelium discoideum, without affecting the expression of cdk5 protein during axenic growth.In vivoRoscovitine, at a dose of 50 mg/kg, significantly inhibits growth of The Ewing\'s sarcoma family of tumors (ESFT) xenografts. Roscovitine enhances the antitumor effect of doxorubicin without increased toxicity with a mechanism that involves cell cycle arrest rather than apoptosis in nude mice bearing established MCF7 xenografts.Cell Datacell lines：Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, Bcr-Abl, or TEL-kinase fusion constructs.Concentrations：0.01 - 100 µMIncubation Time：48 hoursPowder Purity:≥99%