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AG 494

In stock
Catalog No.
B6378
Potent EGFR-kinase inhibitor
Grouped product items
SizePriceStock Qty
10mg
$61.00
In stock
25mg
$146.00
In stock
50mg
$259.00
In stock

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Background

AG 494 is a potent and selective inhibitor of EGFR with IC50 value of 0.7 μM.

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation.

AG 494 is a potent and selective EGFR inhibitor. AG 494 inhibited autophosphorylation of EGFR and HER-2 with IC50 values of 1.1 and 39 μM, respectively. In DHER-14 cells, AG 494 inhibited Cdk2 activation and EGF-dependent DNA synthesis [1]. AG494 arrested cells at late G1 and S phase and inhibited the activation of Cdk2 by phosphorylating tyrosine 15 on Cdk2 [2]. Epidermal growth factor (EGF) increased (bone morphogenetic protein) BMP9-induced osteogenic markers of mesenchymal stem cells (MSCs), which was inhibited by AG-494 in a time- and dose-dependent way [3]. In human prostate (DU145) and lung (A549) cancer cell lines, AG494 reversibly and significantly inhibited autocrine growth in a dose-dependent way. Also, AG494 induced cell apoptosis in both cell lines and arrested cell growth in the G1 phase [4].

References:
[1].  Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett, 1997, 410(2-3): 187-190.
[2].  Kleinberger-Doron N, Shelah N, Capone R, et al. Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase. Exp Cell Res, 1998, 241(2): 340-351.
[3].  Liu X, Qin J, Luo Q, et al. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med, 2013, 17(9): 1160-1172.
[4].  Bojko A1, Reichert K, Adamczyk A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol, 2012, 50(2): 186-195.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt280.28
Cas No.133550-35-3
FormulaC16H12N2O3
SolubilitySoluble in DMSO
Chemical Name(E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-phenylacrylamide
SDFDownload SDF
Canonical SMILESOC1=CC(/C=C(C#N)/C(NC2=CC=CC=C2)=O)=CC=C1O
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.

Quality Control

Quality Control & MSDS

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Chemical structure

AG 494