OSU-03012 (AR-12)

Description: OSU-03012 (also called AR12), a celecoxib derivative without COX-2 inhibitory activity, is an orally bioavailable, specific, and potent inhibitor of recombinant PDK-1 (3-phosphoinositide-dependent kinase-1) with potential antitumor activity. It inhibits PDK-1 with an IC50 of 5 uM in a cell-free assay. OSU-03012 showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo. PDK-1 is a protein in the PI3K/Akt pathway that is involved in the growth and proliferation of cancer cells. AR-12 may also cause cell death through the induction of stress in the endoplasmic reticulum. Currently a multi-centered Phase I clinical study is being carried out using AR-12 in adult patients with advanced or recurrent solid tumors or lymphoma.

References: Cancer Res. 2004 Jun 15; 64(12):4309-18; Cancer Res. 2004 Jun 15; 64(12):4309-18; Mol Pharmacol. 2007 Nov; 72(5):1124-31.

Related CAS #: 1471979-81-3 (HCl)