AG-494

AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM) . AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis[1][2][3].

Product Specifications

CAS Number

[133550-35-3]

Product Name Alternative

Tyrphostin AG 494

UNSPSC

12352005

Hazard Statement

H301, H315, H319

Target

CDK; EGFR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ag-494.html

Purity

98.69

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=CC=C1)/C(C#N)=C/C2=CC=C(O)C(O)=C2

Molecular Formula

C16H12N2O3

Molecular Weight

280.28

Precautions

H301, H315, H319

References & Citations

[1]Gazit A, et al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991;34 (6) :1896-1907.|[2]Liu X, Qin J, 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.|[3]Jihee Lee Kang, et al. SILICA-INDUCED NUCLEAR FACTOR- k B ACTIVATION: INVOLVEMENT OF REACTIVE OXYGEN SPECIES AND PROTEIN TYROSINE KINASE ACTIVATION. Journal of Toxicology and Environmental Health, Part A.|[4]Osherov N, et al. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997;410 (2-3) :187-190.|[5]Osherov N, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem. 1993 May 25;268 (15) :11134-42.