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ACS Med Chem Lett. 2010 May 17;1(5):204-8. doi: 10.1021/ml100051d. eCollection 2010 Aug 12.

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

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1
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033.
2
Merck Research Laboratories, 901 California Avenue, Palo Alto, California 94304.
3
Ligand Pharmaceuticals (formerly Pharmacopeia), 3000 Eastpark Boulevard, Cranbury, New Jersey 08512.

Abstract

Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncology therapeutics. Herein is described the utilization of an in vivo screening approach with integrated efficacy and tolerability parameters to identify candidate CDK inhibitors with a suitable balance of activity and tolerability. This approach has resulted in the identification of SCH 727965, a potent and selective CDK inhibitor that is currently undergoing clinical evaluation.

KEYWORDS:

Cyclin-dependent kinase; SCH 727965; oncology therapeutics

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