Chemical Name: (E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide
Biological ActivityAG 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice.
Abe et al.
Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrophostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
Gazit et al.
Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor.
Meydan et al.
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.
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
PD-L1 blockade enhances response of pancreatic ductal adenocarcinoma to radiotherapy.
Authors: Azad Et al.
EMBO Mol Med 2017;9:167
Let-7 and miR-125 cooperate to prime progenitors for astrogliogenesis.
Authors: Shenoy Et al.
Evodiamine Induces Apoptosis and Inhibits Migration of HCT-116 Human Colorectal Cancer Cells.
Authors: Zhao Et al.
J Transl Med 2015;16:27411
The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling.
Authors: Tactacan Et al.
Mol Cancer 2015;14:139
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
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
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
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.
PLZF is a regulator of homeostatic and cytokine-induced myeloid development.
Authors: Doulatov Et al.
Genes Dev 2009;23:2076
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.
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
IL-9/IL-9 receptor signaling selectively protects cortical neurons against developmental apoptosis.
Authors: Fontaine Et al.
Cell Death Differ 2008;15:1542
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
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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