AG 490

Tocris Bioscience, part of Bio-Techne | Catalog # 0414

COA / SDS

EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor

Key Product Details

Chemical Name:	(E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide
Purity:	≥99%
Molecular Weight:	294.31 kDa

View Full Technical Details for AG 490

Technical Data
Citations

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 kDa
Formula	C₁₇H₁₄N₂O₃
Storage	Store at RT
Purity	≥99%
CAS Number	133550-30-8

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

Solubility

Soluble Soluble to 20 mM in ethanol and to 100 mM in DMSO

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References for AG 490

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

K Qin, K Chen, W Zhao, X Zhao, J Luo, Q Wang, C Gao, X Li, C Wang 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 J Immunol Res, 2018;2018(0):3619320. 2018 PMID: 29670920
Koscso B, Csoka B, Kokai E, Nemeth Z, Pacher P, Virag L, Leibovich S, Hasko G Adenosine augments IL-10-induced STAT3 signaling in M2c macrophages. J Leukoc Biol, 2013;94(6):1309-15. 2013 PMID: 23922379
Fox JT, Sakamuru S, Huang R High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. 2012 PMID: 22431602
Abe et al. The polycythemia vera-associated Jak2 V617F mutant induces tumorigenesis in nude mice. Int.Immunopharmacol., 2009;9:870 PMID: 19327411
Gazit et al. Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrophostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J.Med.Chem., 1991;34:1896 PMID: 1676428
Meydan et al. Inhbition of acute lymphoblastic leukaemia by a JAK-2 inhibitor. Nature, 1996;379:645 PMID: 8628398
Wang 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. J.Immunol., 1999;162:3897 PMID: 10201908