OSU-03012 (AR-12)

- Overview
  - Please contact us at for specific academic pricing.
    
    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].
    
    [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.
- Properties
  - Alternative Name
    
    2-amino-N-[4-[5-phenanthren-2-yl-3-(trifluoromethyl)pyrazol-1-yl]phenyl]acetamide
    
    CAS Number
    
    742112-33-0
    
    Molecular Formula
    
    C26H19F3N4O
    
    Molecular Weight
    
    460.45
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥23 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Dr Jason King. "Katnip, a novel microtubule and autophagy regulator." University of Sheffield December 2020.
    2. Rausch JL, Boichuk S, et al. "Opposing roles of KIT and ABL1 in the therapeutic response of gastrointestinal stromal tumor (GIST) cells to imatinib
    mesylate." Oncotarget. 2017 Jan 17;8(3):4471-4483. PMID:27965460

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OSU-03012 (AR-12)

Background

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