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OSU-03012 (AR-12)

Catalog No.
A2846
Potent PDK1 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$61.00
In stock
5mg
$55.00
In stock
25mg
$176.00
In stock
100mg
$517.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt460.45
Cas No.742112-33-0
FormulaC26H19F3N4O
Solubility≥23 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide
SDFDownload SDF
Canonical SMILESC1=CC=C2C(=C1)C=CC3=C2C=CC(=C3)C4=CC(=NN4C5=CC=C(C=C5)NC(=O)CN)C(F)(F)F
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

PC-3 (p53-/-) human androgen-nonresponsive prostate cancer cells

Preparation method

The solubility of this compound in DMSO is >23mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1, 2.5, 5, 7.5, 10 μM; 6 h

Applications

In PC-3 (p53-/-) human androgen-nonresponsive prostate cancer cells, OSU-03012 reduced the activity of immunoprecipitated p70S6K in a dose-dependent way. OSU-03012 at sub-μM was effective in suppressing PC-3 cell proliferation.

Animal experiment [2]:

Animal models

nude mice bearing established s.c. Huh7 tumor xenografts

Dosage form

100 and 200 mg/kg for 28 days; gavaged

Application

In nude mice bearing established s.c. Huh7 tumor xenografts, OSU-03012 (100 and 200 mg/kg for 28 days) inhibited Huh7 tumor growth by 39.52% and 57.59%, respectively. Compared with vehicle-treated control, OSU-03012 significantly reduced tumor volumes. OSU-03012 induced autophagy in xenograft.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

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          

Quality Control

Chemical structure

OSU-03012 (AR-12)

Related Biological Data

OSU-03012 (AR-12)

Related Biological Data

OSU-03012 (AR-12)

Related Biological Data

OSU-03012 (AR-12)