Cat. No. 0414
Alternative Name: Tyrphostin AG 490
Chemical Name: (E)-2-Cyano-3-(3,4-dihydrophenyl)-N
Biological ActivitySelective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Inhibitor of JAK2, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK pathways and potently inhibits cytokine-independent cell growth in vitro and tumor cell invasion in vivo.
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.
Certificate of Analysis / Safety Data Sheet
Abe et al (2009) The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice. Int.Immunopharmacol. 9 870. PMID: 19327411.
Wang et al (1999) JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response. J.Immunol. 162 3897. PMID: 10201908.
Meydan et al (1996) Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor. Nature 379 645. PMID: 8628398.
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.
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Citations are publications that use Tocris products. Selected citations for AG 490 include:
Tactacan et al (2015) The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling. Mol Cancer 14 139. PMID: 26215634.
Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316. PMID: 25181481.
Jung et al (2008) Reactive oxygen species stabilize hypoxia-inducible factor-1 alpha protein and stimulate transcriptional activity via AMP-activated protein kinase in DU145 human prostate cancer cells. Carcinogenesis 29 713. PMID: 18258605.
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Keywords: AG 490, supplier, JAK2, JAK3, inhibitors, inhibits, EGFR-kinase, JAK, Kinase, Cytokine, NF-κB, NF-kappaB, Signaling, Signalling, Janus, Activated, Kinases, Epidermal, Growth, Factors, Receptors, ErbB, Her, EGFR, RTK, Receptor, Tyrosine, RTKs, AG490, Tyrphostin, AG, 490, Tocris Bioscience, EGFR Inhibitor products
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