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OSU 03012
Axon 2525
CAS:
742112-33-0
Purity:
99%
- Soluble in DMSO
- MF: C26H19F3N4O
- MW: 460.45
Description
ATP-competitive PDK-1 inhibitor (IC50 value 5 μM for both PDK-1/PDPK1) that inhibits the growth of thyroid, prostate and breast cancer xenografts in vivo. A Celecoxib (Axon 1919) derivative that inhibits PAK phosphorylation and cell proliferation with reduced Akt phosphorylation by PDK1, without inhibition of cycloogygenases. Moreover, overexpression of constitutively active forms of PDK-1 and Akt partially protected OSU-03012-induced apoptosis.
More Information
| Parent CAS No. | 742112-33-0 |
|---|---|
| Chemical Name | 2-amino-N-(4-(5-(phenanthren-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)acetamide |
| SMILES | C1C=C2C3=CC=C(C4=CC(C(F)(F)F)=NN4C4C=CC(NC(=O)CN)=CC=4)C=C3C=CC2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C26H19F3N4O/c27-26(28,29)24-14-23(33(32-24)20-10-8-19(9-11-20)31-25(34)15-30)18-7-12-22-17(13-18)6-5-16-3-1-2-4-21(16)22/h1-14H,15,30H2,(H,31,34) |
| InChiKey | YULUCECVQOCQFQ-UHFFFAOYSA-N |
| CID | 10027278 |
| Short Description | PDK-1 inhibitor |
References
- L.M. Porchia et al. 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.
- J. Zhu 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.
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