Biological Activity
Potent, ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) (IC50 = 7 nM). Displays selectivity for mTOR over PI 3-Kα (~100-fold) and PI 3-Kγ (~500-fold). Inhibits phosphorylation of mTORC1 and mTORC2 substrates including S6K, SGK and Akt; blocks VEGF secretion and HIF-1α expression. Exhibits antiproliferative effects in cancer cell lines through G1 cell cycle arrest and selective apoptosis.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries
WYE 687 dihydrochloride 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 | 601.53 |
| Formula | C28H32N8O3 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1062161-90-3 |
| PubChem ID | 90488926 |
| InChI Key | ZQJPHAXLAKKXIX-UHFFFAOYSA-N |
| Smiles | O=C(OC)NC(C=C4)=CC=C4C1=NC(N3CCOCC3)=C2C(N(C5CCN(CC6=CN=CC=C6)CC5)N=C2)=N1.Cl.Cl |
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 | 60.15 | 100 | |
| water | 60.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 601.53. 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 | 1.66 mL | 8.31 mL | 16.62 mL |
| 5 mM | 0.33 mL | 1.66 mL | 3.32 mL |
| 10 mM | 0.17 mL | 0.83 mL | 1.66 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.33 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Yu et al (2009) Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer.Res. 69 6232 PMID: 19584280
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