AG 99

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Cat.No. 0497 - AG 99 | C10H8N2O3 | CAS No. 122520-85-8
Description: EGFR-kinase inhibitor
Chemical Name: (E)-2-Cyano-3-(3,4-dihydroxyphenyl)-2-propenamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Epidermal growth factor receptor (EGFR) kinase inhibitor (IC50 = 10 μM) that is selective over insulin receptor kinase. Blocks tyrosine phosphorylation of p145met 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
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 122520-85-8
PubChem ID 5328768
InChI Key USOXQZNJFMKTKJ-XVNBXDOJSA-N
Smiles NC(=O)C(=C\C1=CC(O)=C(O)C=C1)\C#N

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 1.02 5
DMSO 20.42 100

Preparing Stock Solutions

The following data is based on the product molecular weight 204.18. 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
1 mM 4.9 mL 24.49 mL 48.98 mL
5 mM 0.98 mL 4.9 mL 9.8 mL
10 mM 0.49 mL 2.45 mL 4.9 mL
50 mM 0.1 mL 0.49 mL 0.98 mL

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References

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

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

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

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

Yamamoto et al (2006) Tyrosine phosphorylation of p145met 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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