Biological Activity
Dual Akt and PDK1 inhibitor; binds the pleckstrin homology (PH) domain of Akt and PDK1 (Ki values are 2.7 and 5.2 μM, respectively). Inhibits Akt phosphorylation and Akt downstream targets; also induces apoptosis in vitro. Displays synergistic antitumor effect when combined with chemotherapeutics in breast cancer mouse models.
Compound Libraries
PHT 427 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 409.61 |
| Formula | C20H31N3O2S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1191951-57-1 |
| PubChem ID | 44240850 |
| InChI Key | BYWWNRBKPCPJMG-UHFFFAOYSA-N |
| Smiles | O=S(C(C=C1)=CC=C1CCCCCCCCCCCC)(NC2=NN=CS2)=O |
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 | 40.96 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 409.61. 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 | 2.44 mL | 12.21 mL | 24.41 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.88 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Moses et al (2009) In vitro and in vivo activity of novel small-molecule inhibitors targeting the pleckstrin homology domain of protein kinase B/AKT. Cancer Res. 69 5073 PMID: 19491272
Meuillet et al (2010) Molecular pharmacology and antitumor activity of PHT-427, a novel Akt/phosphatidylinositide-dependent protein kinase 1 pleckstrin homology domain inhibitor. Mol.Cancer Ther. 9 706 PMID: 20197390
Keywords: PHT 427, supplier, PHT427, Phosphatidylinositol, 3-kinase/phosphatidylinositide-dependent, protein, kinase, 1, PDPK1Akt,, pleckstrin, homology, PH, domain, AKT, inhibitors, inhibits, antitumor, duel, tumour, PDK1, Akt, (Protein, Kinase, B), Protein, Kinase, B/Akt, PDK1, Phosphoinositide-dependent, Kinase, 1, Akt, (Protein, Kinase, B), Tocris Bioscience
