AG 490
Chemical Name: (E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide
Purity: ≥99%
Biological Activity
AG 490 is a 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
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.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Adenosine augments IL-10-induced STAT3 signaling in M2c macrophages.
Koscso B, Csoka B, Kokai E, Nemeth Z, Pacher P, Virag L, Leibovich S, Hasko G
J Leukoc Biol, 2013;94(6):1309-15. -
Methotrexate Combined with 4-Hydroperoxycyclophosphamide Downregulates Multidrug-Resistance P-Glycoprotein Expression Induced by Methotrexate in Rheumatoid Arthritis Fibroblast-Like Synoviocytes via the JAK2/STAT3 Pathway
K Qin, K Chen, W Zhao, X Zhao, J Luo, Q Wang, C Gao, X Li, C Wang
J Immunol Res, 2018;2018(0):3619320. -
PD-L1 blockade enhances response of pancreatic ductal adenocarcinoma to radiotherapy
EMBO Mol Med, 2016;0(0):. -
The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice.
Abe et al.
Int.Immunopharmacol., 2009;9:870 -
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 -
Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor.
Meydan et al.
Nature, 1996;379:645 -
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
Product Datasheets
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Citations for AG 490
The citations listed below are publications that use Tocris products. Selected citations for AG 490 include:
14 Citations: Showing 1 - 10
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PD-L1 blockade enhances response of pancreatic ductal adenocarcinoma to radiotherapy.
Authors: Azad Et al.
EMBO Mol Med 2017;9:167
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Let-7 and miR-125 cooperate to prime progenitors for astrogliogenesis.
Authors: Shenoy Et al.
Neuropsychopharmacology 2015;34:1180
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Evodiamine Induces Apoptosis and Inhibits Migration of HCT-116 Human Colorectal Cancer Cells.
Authors: Zhao Et al.
J Transl Med 2015;16:27411
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The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling.
Authors: Tactacan Et al.
Mol Cancer 2015;14:139
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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
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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
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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
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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
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PLZF is a regulator of homeostatic and cytokine-induced myeloid development.
Authors: Doulatov Et al.
Genes Dev 2009;23:2076
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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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JAK/STAT and PI3K/AKT pathways form a mutual transactivation loop and afford resistance to oxidative stress-induced apoptosis in cardiomyocytes.
Authors: Lu Et al.
Cell Physiol Biochem 2008;21:305
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IL-9/IL-9 receptor signaling selectively protects cortical neurons against developmental apoptosis.
Authors: Fontaine Et al.
Cell Death Differ 2008;15:1542
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The JAK/STAT pathway is essential for opioid-induced cardioprotection: JAK2 as a mediator of STAT3, Akt, and GSK-3 beta.
Authors: Gross Et al.
Am J Physiol Heart Circ Physiol 2006;291:H827
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Intracellular pathways triggered by the selective FLT-1-agonist placental growth factor in vascular smooth muscle cells exposed to hypoxia.
Authors: Bellik Et al.
Br J Pharmacol 2005;146:568
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