Biological Activity
Selective inhibitor of the epidermal growth factor receptor (EGFR) (IC50 = 0.3 μM in vitro). Also inhibits and reverses the formation of Aβ42 fibers associated with Alzheimer's disease. Eliminates calcium influx potential when coincubated with amyloid β-peptide (1-42) (Cat.No. 1428); reduces neurotoxicity by blocking Ca2+ influx into neuronal cells.
Compound Libraries
CGP 52411 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 329.35 |
| Formula | C20H15N3O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 145915-58-8 |
| PubChem ID | 1697 |
| InChI Key | AAALVYBICLMAMA-UHFFFAOYSA-N |
| Smiles | O=C2NC(C1=CC(NC4=CC=CC=C4)=C(NC3=CC=CC=C3)C=C12)=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 | 32.94 | 100 | |
| ethanol | 8.23 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 329.35. 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 | 3.04 mL | 15.18 mL | 30.36 mL |
| 5 mM | 0.61 mL | 3.04 mL | 6.07 mL |
| 10 mM | 0.3 mL | 1.52 mL | 3.04 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.61 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Buchdunger et al (1994) 4,5-dianilinophthalimide: a protein tyrosine kinase inhibitor with selectivity for the epidermal growth factor receptor signal transduction pathway and potent in vivo antitumor activity. Proc.Natl.Acad.Sci. 91 2334 PMID: 8134396
Blanchard et al (2004) Efficient reversal of Alzheimer's disease fibril formation and elimination of neurotoxicity by a small molecule. Proc.Natl.Acad.Sci. 101 14326 PMID: 15388848
Wang et al (2008) Direct and selective elimination of specific prions and amyloids by 4,5-dianilinophthalimide and analogs. Proc.Natl.Acad.Sci. 105 7159 PMID: 18480256
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