OSU-03012 | CAS:742112-33-0

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Name:OSU-03012; AR-12
Cat. No. :CS-0151
CAS No. :742112-33-0
Formula:C26H19F3N4O
M. Wt. : 460.45
Solubility:10 mM in DMSO

OSU-03012 is a PDK-1 inhibitor with an IC50 of 5 μM.IC50 & Target: IC50: 5 μM (PDK-1)[1]In Vitro: OSU-03012 inhibits PC-3 cells viability with IC50 values of 5 μM. The effects of OSU-03012 on PC-3 cell proliferation in 10% FBS-supplemented medium are also examined. OSU-03012 induces apoptotic death in PC-3 cells in 1% FBS-containing medium in a dose-dependent manner, as demonstrated by DNA fragmentation and PARP cleavage. OSU-03012 is effective in suppressing PC-3 cell proliferation at sub-μM, consistent with that noted in 1% serum[1].In Vivo: All of the SCID/Rag2 mice develop two MDA-MB-435/LCC6/Her-2 tumors and are assigned to either the vehicle control or OSU-03012 (200 mg/kg) treatment group, which is given orally for 3 days. OSU-03012 remarkably decreases EGFR protein expression in the tumors by ~48% compared with expression levels found in the tumors taken from mice that receive the vehicle control. OSU-03012 also prevents Y-box binding protein-1 (YB-1) from binding to the EGFR promoter at the 1b and 2a sites[2].

To K, et al. The phosphoinositide-dependent kinase-1 inhibitor 2-amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-acetamide (OSU-03012) prevents Y-box binding protein-1 from inducing epidermal growth factor receptor. Mol Pharmacol. 2007 Sep;72(3):641-52. Zhu J, et al. From the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 2004 Jun 15;64(12):4309-18.