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Submit ReviewAG 490
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)
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 Data 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 | 3.4 mL | 16.99 mL | 33.98 mL |
| 5 mM | 0.68 mL | 3.4 mL | 6.8 mL |
| 10 mM | 0.34 mL | 1.7 mL | 3.4 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
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Product Datasheets for AG 490
References for AG 490
References are publications that support the biological activity of the product.
Abe et al (2009) The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice. Int.Immunopharmacol. 9 870 PMID: 19327411
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
Meydan et al (1996) Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor. Nature 379 645 PMID: 8628398
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
If you know of a relevant reference for AG 490, please let us know.
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Keywords: AG 490, 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, 0414, Tocris Bioscience
14 Citations for AG 490
Citations are publications that use Tocris products. Selected citations for AG 490 include:
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
Tactacan et al (2015) The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling. Mol Cancer 14 139 PMID: 26215634
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
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
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
Azad et al (2017) PD-L1 blockade enhances response of pancreatic ductal adenocarcinoma to radiotherapy. EMBO Mol Med 9 167 PMID: 27932443
Doulatov et al (2009) PLZF is a regulator of homeostatic and cytokine-induced myeloid development. Genes Dev 23 2076 PMID: 19723763
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
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
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