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OSU-03012 (AR-12)

potent PDK-1 inhibitor

OSU-03012 (AR-12)

Catalog No. A2846
Size Price Stock Qty
5mg $50.00 In stock
25mg $120.00 In stock
100mg $490.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

OSU-03012 (AR-12)

Biological Activity

Description OSU-03012 is potent inhibitor of recombinant PDK-1 with IC50 value of 5 μM.
Targets recombinant PDK-1          
IC50 5 μM          

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Chemical Properties

Cas No. 742112-33-0 SDF Download SDF
Chemical Name 2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide
Canonical SMILES C1=CC=C2C(=C1)C=CC3=C2C=CC(=C3)C4=CC(=NN4C5=CC=C(C=C5)NC(=O)CN)C(F)(F)F
Formula C26H19F3N4O M.Wt 460.45
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

OSU-03012 (AR-12) is an inhibitor of 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 value of 5μm, which shows 2-fold higher potency over OSU-02067 [1].

OSU-03012 has represented to suppress PC-3 cell proliferation and induce apoptosis in PC-3 cells. Expression of the constitutively active forms of PDK-1 and Akt has revealed to reduce OSU-03012-induced apoptosis in PC-3 cell [1].

OSU-03012 could potently inhibit the growth of primary human VS cells and malignant schwannoma HMS-97 cells in a dose-dependent manner. In contrast, normal human Schwann cells showed to be more resistant to OSU-03012. Additionally, OSU-03012 revealed to inhibit phosphorylation of AKT at the threonine-308 site in both VS cells and HMS-97 cells [2].

References:
[1] Zhu J1, Huang JW, Tseng PH, Yang YT, Fowble J, Shiau CW, Shaw YJ, Kulp SK, Chen CS. 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.
[2] Lee TX1, Packer MD, Huang J, Akhmametyeva EM, Kulp SK, Chen CS, Giovannini M, Jacob A, Welling DB, Chang LS. Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer. 2009 Jun;45(9):1709-20.