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AG-490

In stock
Catalog No.
A4139
JAK2/EGFR inhibitor
Grouped product items
SizePriceStock Qty
25mg
$60.00
In stock

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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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt294.3
Cas No.133550-30-8
FormulaC17H14N2O3
SynonymsTyrphostin B42
Solubility≥14.7 mg/mL in DMSO, ≥4.73 mg/mL in EtOH with ultrasonic and warming, <2.56 mg/mL in H2O
Chemical Name(E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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      

Quality Control

Chemical structure

AG-490

Related Biological Data

AG-490

Related Biological Data

AG-490