742112-33-0

溶解度:Soluble in DMSO

储存条件:-20C 2 years

生物活性

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. ^[1]
OSU-03012 inhibited cell proliferation more effectively in both VS (IC50=3.1 μM ) and HMS-97 (IC50=2.6 μM )cells than in normal human Schwann cells(IC50=12 μM ).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.

参考文献

[1] Lee TX et al. Eur J Cancer. 2009 Jun;45(9):1709-20