OSU03012

OSU03012 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.^1,2,3 It has an IC₅₀ value of 5 µM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM.² OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 µM across a panel of 60 cancer cell lines.² It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway.³ OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.¹

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1. Johnson, A.J., Smith, L.L., Zhu, J., et al. A novel celecoxib derivative, OSU03012, induces cytotoxicity in primary CLL cells and transformed B-cell lymophoma cell line via a caspase- and Bcl-2-independent mechanism. Blood 105(6), 2504-2509 (2005).

2. Zhu, J., Huang, J.W., Tseng, P.H., et al. From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 64, 4309-4318 (2004).

3. Kucab, J.E., Lee, C., Chen, C.S., et al. Celecoxib analogues disrupt Akt signaling, which is commonly activated in primary breast tumors. Breast Cancer Res. 7(5), R796-R807 (2004).