AG 490

Tocris Bioscience a Bio-Techne Brand

Catalog # 0414

Citations (14)

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Key Product Details

Description:	EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor
Alternative Names:	Tyrphostin AG 490
Chemical Name:	(E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide
Purity:	≥99% (HPLC)
Molecular Weight:	294.31

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Biological Activity for AG 490

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 for AG 490

M. Wt	294.31
Formula	C₁₇H₁₄N₂O₃
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	133550-30-8
PubChem ID	5328779
InChi Key	TUCIOBMMDDOEMM-RIYZIHGNSA-N
Smiles	OC1=C(O)C=C(\C=C(/C#N)C(=O)NCC2=CC=CC=C2)C=C1

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.

Solubility for AG 490

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	5.89	20
	DMSO	29.43	100

Preparing Stock Solutions for AG 490

The following data is based on the product molecular weight 294.31.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.40 mL	16.99 mL	33.98 mL
5 mM	0.68 mL	3.40 mL	6.80 mL
10 mM	0.34 mL	1.70 mL	3.40 mL
50 mM	0.07 mL	0.34 mL	0.68 mL

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References for AG 490

References are publications that support the biological activity of the product.

Abe The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice. Int.Immunopharmacol. 2009 PMID: 19327411
Wang 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. 1999 PMID: 10201908
Meydan Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor. Nature 1996 PMID: 8628398
Gazit Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrophostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J.Med.Chem. 1991 PMID: 1676428

Citations for AG 490 (14)

Showing 1 - 10 of 14 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for AG 490 include:

Azad et al. (2017) PD-L1 blockade enhances response of pancreatic ductal adenocarcinoma to radiotherapy. EMBO Mol Med. 9:167
PMID: 27932443
Tactacan et al. (2015) The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling. Mol Cancer. 14:139
PMID: 26215634
Zhao et al. (2015) Evodiamine Induces Apoptosis and Inhibits Migration of HCT-116 Human Colorectal Cancer Cells. J Transl Med. 16:27411
PMID: 26580615
Jiang et al. (2015) YangZheng XiaoJi exerts anti-tumour growth effects by antagonising the effects of HGF and its receptor, cMET, in human lung cancer cells. PLoS One. 13:280
PMID: 26310485
Shenoy et al. (2015) Let-7 and miR-125 cooperate to prime progenitors for astrogliogenesis. Neuropsychopharmacology. 34:1180
PMID: 25715649
Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. EMBO J. 10:e0143319
PMID: 26619345
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
Park et al. (2013) Inactivation of JAK2/STAT3 signaling axis and downregulation of M1 mAChR cause cognitive impairment in klotho mutant mice, a genetic model of aging. Neuron. 38:1426
PMID: 23389690
Doulatov et al. (2009) PLZF is a regulator of homeostatic and cytokine-induced myeloid development. Genes Dev. 23:2076
PMID: 19723763
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
Fontaine et al. (2008) IL-9/IL-9 receptor signaling selectively protects cortical neurons against developmental apoptosis. Cell Death Differ. 15:1542
PMID: 18551134
Lu et al. (2008) JAK/STAT and PI3K/AKT pathways form a mutual transactivation loop and afford resistance to oxidative stress-induced apoptosis in cardiomyocytes. Cell Physiol Biochem. 21:305
PMID: 18441519
Gross et al. (2006) The JAK/STAT pathway is essential for opioid-induced cardioprotection: JAK2 as a mediator of STAT3, Akt, and GSK-3 beta. Am J Physiol Heart Circ Physiol. 291:H827
PMID: 16517948
Bellik et al. (2005) Intracellular pathways triggered by the selective FLT-1-agonist placental growth factor in vascular smooth muscle cells exposed to hypoxia. Br J Pharmacol. 146:568
PMID: 16086034

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Showing 1 - 10 of 14 citations Showing All

Product Documents for AG 490

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.