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AG 99

Cat. No. 0497

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Chemical Name: (E)-2-Cyano-3-(3,4-dihydroxyphenyl)-2-propenamide

Biological Activity

Epidermal growth factor receptor (EGFR) kinase inhibitor (IC₅₀ = 10 μM) that is selective over insulin receptor kinase. Blocks tyrosine phosphorylation of p145^met and promotes cell death of normal and cancer cells via activation of caspase-like proteases in vitro.

Technical Data

M.Wt:

204.18

Formula:

C₁₀H₈N₂O₃

Solubility:

Soluble to 5 mM in ethanol and to 100 mM in DMSO

Purity:

>99 %

Storage:

Desiccate at +4°C

CAS No:

122520-85-8

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

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Gazit et al (1989) Tyrphostins. I. Synthesis and biological activity of protein tyrosine kinase inhibitors. J.Med.Chem. 32 2344. PMID: 2552117.

Levitzki and Gilon (1991) Tyrphostins as molecular tools and potential antiproliferative drugs. TiPS 12 171. PMID: 1862529.

Gazit (1996) Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrphostins: potent inhibitors of EGF receptor tyrosine kinase in vitro. J.Med.Chem. 39 4905. PMID: 8960549.

Yamamoto et al (2006) Tyrosine phosphorylation of p145^met mediated by EGFR and Src is required for serum-independent survival of human bladder carcinoma cells. J.Cell Sci. 119 4623. PMID: 17062641.

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