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PDK1 inhibitor AR12

Chemical Structure : PDK1 inhibitor AR12

CAS No.: 742112-33-0

PDK1 inhibitor AR12 (AR-12, OSU-03012, OSU03012)

Catalog No.: PC-60605Not For Human Use, Lab Use Only.

OSU-03012 (AR12) is a potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) inhibitor with IC50 of 5 uM.

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Biological Activity

OSU-03012 (AR12) is a potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) inhibitor with IC50 of 5 uM.
OSU-03012 induces apoptosis in PC-3 cells at low microM range, causes Akt dephosphorylation and inhibition of p70 S6 kinase activity;.
OSU-03012 displays cytotocixity against a panel of 60 cell lines with mean GI50 of 3 uM.
OSU-03012 decreases incidences of carcinoma and metastasis in transgenic mouse model of prostate cancer.

Physicochemical Properties

M.Wt 460.46
Formula C26H19F3N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-phenyl} acetamide

References

1. Johnson AJ, et al. Blood. 2005 Mar 15;105(6):2504-9.

2. Tseng PH, et al. Blood. 2005 May 15;105(10):4021-7.

3. Zhu J, et al. Cancer Res. 2004 Jun 15;64(12):4309-18.

4. Baryawno N, et al. Cancer Res. 2010 Jan 1;70(1):266-76.

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