AG 490

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Synonyms: 2-Cyano-3-(3,4-dihydroxyphenyl)-N-(phenylmethyl)-2-propenamide, 2-Cyano-3-(3,4-dihydroxyphenyl)-N-(benzyl)-2-propenamide, Tyrphostin AG 490

IUPAC Name:

(E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide

Functional Activity:

Selective inhibitor of EGF receptor tyrosine kinase. It also potently inhibits JAK2, JAK3 pathways and cytokine-independent cell growth in vitro and tumor cell invasion in vivo.

Technical Data:

M.Wt: 294.30

Formula: C₁₇H₁₄N₂O₃

Solubility: Soluble in DMSO and ethanol

Purity: >97%

Storage: Dessicate at -20°C

CAS No.: 133550-30-8

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References for AG 490

1. Seo, I. A., Lee, H. K., Shin, Y. K., Lee, S. H., Seo, S. Y., Park, J. W., and Park, H. T. Janus Kinase 2 Inhibitor AG490 Inhibits the STAT3 Signaling Pathway by Suppressing Protein Translation of gp130. Korean J Physiol Pharmacol, 13: 131-138, 2009.

2. Wu, M. H., Chen, X. Y., and Cai, K. R. Effects of a JAK inhibitor, AG490, on proliferation and apoptosis of human nasopharyngeal carcinoma cell line CNE-2Z. Ai Zheng, 28: 24-28, 2009.

3. Tsuchiya, Y., Takahashi, N., Yoshizaki, T., Tanno, S., Ohhira, M., Motomura, W., Tanno, S., Takakusaki, K., Kohgo, Y., and Okumura, T. A Jak2 inhibitor, AG490, reverses lipin-1 suppression by TNF-alpha in 3T3-L1 adipocytes. Biochem Biophys Res Commun, 382: 348-352, 2009.

4. Caceres-Cortes, J. R. A potent anti-carcinoma and anti-acute myeloblastic leukemia agent, AG490. Anticancer Agents Med Chem, 8: 717-722, 2008.

5. Kwak, H. B., Sun, H. M., Ha, H., Lee, J. H., Kim, H. N., and Lee, Z. H. AG490, a Jak2-specific inhibitor, induces osteoclast survival by activating the Akt and ERK signaling pathways. Mol Cells, 26: 436-442, 2008.

6. Chen, H. F., Deng, H. Y., and Fan, W. K. [Effect of Janus kinase inhibitor AG490 on invasion and metastasis of human breast cancer cells]. Sichuan Da Xue Xue Bao Yi Xue Ban, 39: 63-65, 83, 2008.

Certificate of Analysis/MSDS is available upon request with lot number