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AG-490JAK2/EGFR inhibitor

AG-490

Catalog No. A4139
Size Price Stock Qty
10mg $30.00 In stock
25mg $60.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AG-490

Biological Activity

Description AG-490 is a tyrosine kinase inhibitor of JAK2, EGFR, and ErbB2 with IC50 values of ~10 μM, 0.1 μM and 13.5 μM, respectively.
Targets JAK2 EGFR ErbB2      
IC50 ~10 μM 0.1 μM 13.5 μM      

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Chemical Properties

Cas No. 133550-30-8 SDF Download SDF
Chemical Name (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
Canonical SMILES C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N
Formula C17H14N2O3 M.Wt 294.3
Solubility >14.7mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

AG-490 is an inhibitor of tyrosine kinases [1].

As a member of the tyrphostin family, AG-490 is reported to have inhibitory activity against many kinases. It can inhibit the hyperactive JAK2 in B cell precursors of ALL patients, inhibit cytokine-induced activation of JAK2 in eosinophils and suppresses the activation of STAT3 in mycosis fungoides-derived T cells. AG-490 is also found to target JAK3 and its downstream STAT and MAPK signaling pathways. In the IL-2-dependent T cell line, D10, AG-490 suppresses IL-2-induced cell proliferation with IC50 value of 25μM without affecting IL-2R chain expression. It also inhibits IL-2-modulated phosphorylation of STAT5a and STAT5b with IC50 value of 50μM-70μM. Moreover, AG-490 reduces IL-2-induced DNA binding by 78%, 65% and 65% for STAT5a/5b, STAT1 and STAT3, respectively. All these show that AG-490 may provide a beneficial therapeutic by suppressing immunopathological states [1].

References:
[1] Wang L H, Kirken R A, Erwin R A, 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. The Journal of Immunology, 1999, 162(7): 3897-3904.