Biological Activity
ERK dimerization inhibitor (IC50 ~ 0.5 μM); inhibits ERK dimerization without affecting phosphorylation or kinase activity. Suppresses growth of tumor cells expressing RAS-ERK oncogenes in vitro. Induces apoptosis and prevents tumor progression in vivo.
Technical Data
| M. Wt | 444.53 |
| Formula | C26H28N4O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 181223-80-3 |
| PubChem ID | 11224574 |
| InChI Key | INQUULPXCZAKMS-XKZIYDEJSA-N |
| Smiles | O=C1NC2=CC=C(NC(CCN3CCCCC3)=O)C=C2/C1=C/C4=CNC5=C4C=C(OC)C=C5 |
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 | 22.23 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 444.53. 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 | 2.25 mL | 11.25 mL | 22.5 mL |
| 5 mM | 0.45 mL | 2.25 mL | 4.5 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.25 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Herrero et al (2015) Small molecule inhibition of ERK dimerization prevents tumorigenesis by RAS-ERK pathway oncogenes. Cancer Cell 28 170 PMID: 26267534
Ryan et al (2015) Targeting RAS-mutant cancers: is ERK the key? Trends Cancer 1 183 PMID: 26858988
Keywords: DEL 22379, supplier, ERK, dimerization, inhibitors, inhibits, extracellular, signal, related, kinase, RAS, ERK, ERK, Tocris Bioscience
