Home >> AG-490
Related Products
AG-490 JAK2/EGFR inhibitor

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

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Product Citations

1. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
2. Wang L, Zhang F, et al. "CAFs enhance paclitaxel resistance by inducing EMT through the IL‑6/JAK2/STAT3 pathway." Oncol Rep. 2018 May;39(5):2081-2090. PMID:29565447

Quality Control

Chemical structure

AG-490

Related Biological Data

AG-490

Related Biological Data

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      

AG-490 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

AG-490 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 133550-30-8 SDF Download SDF
Synonyms N/A
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
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For 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.

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.