OSU-03012 is a recently licensed novel derivative of the cyclooxygenase-2 (COX-2) inhibitor celecoxib (CelebrexTM); however, it lacks COX-2 inhibitory activity. It potently induces apoptosis in several types of cancer cells.The mechanism is mediated, at least in part, through the inhibition of phosphoinositide-dependent kinase-1 (PDK-1), an upstream kinase that phosphorylates AKT.OSU-03012 inhibited cell proliferation more effectively in both VS (IC50=3.1 ¦ÌM ) and HMS-97 (IC50=2.6 ¦ÌM )cells than in normal human Schwann cells(IC50=12 ¦ÌM ). OSU-03012 was well tolerated and inhibited the growth of HMS-97 schwannoma xenografts by 55% after 9 weeks of oral treatment. The anti-tumour activity correlated with reduced AKT phosphorylation

June 21, 2017

prudect name : OSU-03012 is a recently licensed novel derivative of the cyclooxygenase-2 (COX-2) inhibitor celecoxib (CelebrexTM); however, it lacks COX-2 inhibitory activity. It potently induces apoptosis in several types of cancer cells.The mechanism is mediated, at least in part, through the inhibition of phosphoinositide-dependent kinase-1 (PDK-1), an upstream kinase that phosphorylates AKT.OSU-03012 inhibited cell proliferation more effectively in both VS (IC50=3.1 ¦ÌM ) and HMS-97 (IC50=2.6 ¦ÌM )cells than in normal human Schwann cells(IC50=12 ¦ÌM ). OSU-03012 was well tolerated and inhibited the growth of HMS-97 schwannoma xenografts by 55% after 9 weeks of oral treatment. The anti-tumour activity correlated with reduced AKT phosphorylation
OSU-03012

Synonyms: CAS NO: 742112-33-0Molecular Formula: C26H19F3N4OMolecular Weight: 460.45Purity: 98%Solubility: In DMSOStorage: -20°C


web site: www.medchemexpress.com

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18538357