Catalog Number: 0414
Alternate Names: Tyrphostin AG 490
Chemical Name: (E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide
Biological Activity
Selective 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.
Technical Data
  • M.Wt:
    294.31
  • Formula:
    C17H14N2O3
  • Solubility:
    Soluble to 20 mM in ethanol and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    133550-30-8
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.
Background References
  1. The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice.
    Abe et al.
    Int.Immunopharmacol., 2009;9:870
  2. Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrophostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
    Gazit et al.
    J.Med.Chem., 1991;34:1896
  3. Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor.
    Meydan et al.
    Nature, 1996;379:645
  4. JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response.
    Wang et al.
    J.Immunol., 1999;162:3897
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AG 490 include:

8 Citations: Showing 1 - 8
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  1. Let-7 and miR-125 cooperate to prime progenitors for astrogliogenesis.
    Authors: Shenoy Et al.
    Neuropsychopharmacology 2015;34:1180
  2. Evodiamine Induces Apoptosis and Inhibits Migration of HCT-116 Human Colorectal Cancer Cells.
    Authors: Zhao Et al.
    J Transl Med 2015;16:27411
  3. The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling.
    Authors: Tactacan Et al.
    Mol Cancer 2015;14:139
  4. YangZheng XiaoJi exerts anti-tumour growth effects by antagonising the effects of HGF and its receptor, cMET, in human lung cancer cells.
    Authors: Jiang Et al.
    PLoS One 2015;13:280
  5. Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways.
    Authors: Rogers and Gahring
    EMBO J 2015;10:e0143319
  6. mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
    Authors: Kubota Et al.
    PLoS One 2014;9:e106316
  7. Inactivation of JAK2/STAT3 signaling axis and downregulation of M1 mAChR cause cognitive impairment in klotho mutant mice, a genetic model of aging.
    Authors: Park Et al.
    Neuron 2013;38:1426
  8. 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.
    Authors: Jung Et al.
    Carcinogenesis 2008;29:713

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