AG 494

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Cat.No. 0619 - AG 494 | C16H12N2O3 | CAS No. 133550-35-3
Description: Potent EGFR-kinase inhibitor
Chemical Name: (E)-2-Cyano-3-(3,4-dihydroxyphenyl)-N-phenyl-2-propenamide
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent inhibitor of epidermal growth factor receptor (EGFR) kinase (IC50 = 0.7 μM). Selective over ErbB2, PDGFR and insulin receptor kinase (IC50 values are 42, 6 and > 100 μM respectively).

Technical Data

M. Wt 280.28
Formula C16H12N2O3
Storage Desiccate at +4°C
CAS Number 133550-35-3
PubChem ID 5328771
InChI Key HKHOVJYOELRGMV-XYOKQWHBSA-N
Smiles OC1=C(O)C=C(\C=C(/C#N)C(=O)NC2=CC=CC=C2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 1.4 5
DMSO 14.01 50

Preparing Stock Solutions

The following data is based on the product molecular weight 280.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 7.14 mL 35.68 mL 71.36 mL
2.5 mM 1.43 mL 7.14 mL 14.27 mL
5 mM 0.71 mL 3.57 mL 7.14 mL
25 mM 0.14 mL 0.71 mL 1.43 mL

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References

References are publications that support the biological activity of the product.

Ben-Bassat et al (1999) Tyrphostins that suppress the growth of human papilloma virus 16-immortalized human keratinocytes. J.Pharmacol.Exp.Ther. 290 1442 PMID: 10454524

Gazit et al (1991) Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrophostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J.Med.Chem. 34 1896 PMID: 1676428

Tomlins et al (2005) Cross-talk between the calcium-sensing receptor and the epidermal growth factor receptor in Rat-1 fibroblasts. Exp.Cell Res. 308 439 PMID: 15950968


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