Biological Activity
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
OSU 03012 is also offered as part of the Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.05 | 100 | |
| ethanol | 9.21 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 460.45. Batch specific molecular weights may vary from batch to batch due to solvent 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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 celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. Cancer Res. 64 4309 PMID: 15205346
Keywords: OSU 03012, supplier, OSU03012, PDK1, Akt, antitumor, anticancer, 3-phospho-inositide-dependent, kinases-1, PDPK1, Phosphoinositide-dependent, Kinase, 1, PDK1, Akt, (Protein, Kinase, B), Protein, Kinase, B/Akt, Phosphoinositide-dependent, Kinase, 1, Tocris Bioscience
