REVIEW OSU-03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway. It is a potent inhibitor of tumor cell growth and induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.
REFERENCES
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Porchia LM, Guerra M, Wang YC, Zhang Y, Espinosa AV, Shinohara M, Kulp SK, Kirschner LS, Saji M, Chen CS, Ringel MD. 2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-phenyl} acetamide (OSU-03012), a celecoxib derivative, directly targets p21-activated kinase. Mol Pharmacol. (2007) Nov;72(5): 1124-31.
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Zhang S, Suvannasankha A, Crean CD, White VL, Johnson A, Chen CS, Farag SS. OSU-03012, a novel celecoxib derivative, is cytotoxic to myeloma cells and acts through multiple mechanisms. Clin Cancer Res. (2007) Aug 15;13(16): 4750-8.
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McCubrey, James A.; LaHair, Michelle M.; Franklin, Richard A. OSU-03012 in the treatment of glioblastoma. Molecular Pharmacology. (2006) 70(2): 437-439.
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Zhu, Jiuxiang; Huang, Jui-Wen; Tseng, Ping-Hui; Yang, Ya-Ting; Fowble, Joseph; Shiau, Chung-Wai; Shaw, Yeng-Jeng; Kulp, Samuel K.; Chen, Ching-Shih From the Cyclooxygenase-2 Inhibitor Celecoxib to a Novel Class of 3-Phosphoinositide-Dependent Protein Kinase-1 Inhibitors Cancer Research (2004), 64(12), 4309-4318
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