Brief Description |
Dinaciclib (SCH 727965) is a potent and selective CDK inhibitor and a novel cytotoxic agent. It inhibits CDK2, CDK5, CDK1, and CDK9 activity in vitro with IC50 values of 1, 1, 3, and 4 nM, respectively. It exhibits superior activity, compared with flavopiridol, with a much improved therapeutic index. It is currently in clinical trials. |
References |
1. D. Parry, et al, Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor, Mol Cancer Ther, 2010, 9(8); 2344-53
2. K. Paruch, et al, Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases, ACS Med. Chem. Lett., 2010, 1 (5), pp 204-208
3. G. Feldmann, et al, Cyclin-dependent kinase inhibitor Dinaciclib (SCH727965) inhibits pancreatic cancer growth and progression in murine xenograft models, Cancer Biol. Ther. 2011, 12(7), 598-609 |