OSU 03012

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Description: PDPK1 (PDK1) inhibitor; inhibits Akt signaling
Chemical Name: 2-Amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]acetamide
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for OSU 03012

OSU 03012 is a PDPK1 (PDK1) inhibitor; inhibits Akt signaling. Induces apoptosis of PC-3 and medulloblastoma cells, and inhibits growth of a number of tumor cell lines. Sensitizes radiotherapy-induced cell death and enhances cytotoxic effects of chemotherapeutic agents in vitro. Attenuates tumor growth of medulloblastoma xenografts in mice.

Compound Libraries for OSU 03012

OSU 03012 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for OSU 03012

M. Wt 460.45
Formula C26H19F3N4O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 742112-33-0
PubChem ID 10027278
Smiles O=C(CN)NC(C=C1)=CC=C1N2C(C(C=C3)=CC4=C3C5=CC=CC=C5C=C4)=CC(C(F)(F)F)=N2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for OSU 03012

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 46.05 100

Preparing Stock Solutions for OSU 03012

The following data is based on the product molecular weight 460.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.17 mL 10.86 mL 21.72 mL
5 mM 0.43 mL 2.17 mL 4.34 mL
10 mM 0.22 mL 1.09 mL 2.17 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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References for OSU 03012

References are publications that support the biological activity of the product.

Baryawno et al (2010) Small-molecule inhibitors of phosphatidylinositol 3-kinase/Akt signaling inhibit Wnt/β-catenin pathway cross-talk and suppress medulloblastoma growth. Cancer Res. 70 266 PMID: 20028853

Yacoub et al (2006) OSU-03012 promotes caspase-independent but PERK-, cathepsin B-, BID-, and AIF-dependent killing of transformed cells. Mol.Pharmacol. 70 589 PMID: 16622074

Zhu et al (2004) From the cyclooxygenase-2 inhibitor cele. to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 64 4309 PMID: 15205346

If you know of a relevant reference for OSU 03012, please let us know.

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Keywords: OSU 03012, OSU 03012 supplier, OSU03012, PDK1, Akt, antitumor, anticancer, 3-phospho-inositide-dependent, kinases-1, PDPK1, Phosphoinositide-dependent, Kinase, 1, (Protein, B), Protein, B/Akt, 5682, Tocris Bioscience

1 Citation for OSU 03012

Citations are publications that use Tocris products. Selected citations for OSU 03012 include:

Hye Jung et al (2022) P2Y2R-Mediated PAK1 Activation Is Involved in ESM-1 Overexpression in RT-R-MDA-MB-231 through FoxO1 Regulation. Cancers (Basel) 14 PMID: 36077661

Do you know of a great paper that uses OSU 03012 from Tocris? Please let us know.

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