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Submit ReviewOSU 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.
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.
M. Wt | 460.45 |
Formula | C26H19F3N4O |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 742112-33-0 |
PubChem ID | 10027278 |
InChI Key | YULUCECVQOCQFQ-UHFFFAOYSA-N |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 46.05 | 100 |
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.
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 |
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.
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
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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