AG-494

Modify Date: 2024-01-06 22:52:54

AG-494 Structure
AG-494 structure
Common Name AG-494
CAS Number 133550-35-3 Molecular Weight 280.278
Density 1.4±0.1 g/cm3 Boiling Point 586.9±50.0 °C at 760 mmHg
Molecular Formula C16H12N2O3 Melting Point 249 °C(dec.)
MSDS N/A Flash Point 308.8±30.1 °C

 Use of 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].

 Names

Name 2-cyano-3-(3,4-dihydroxyphenyl)-N-phenylprop-2-enamide
Synonym More Synonyms

 AG-494 Biological Activity

Description 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].
Related Catalog
Target

EGFR:0.7 μM (IC50)

In Vitro In DHER-14 cells, AG 494 inhibits Cdk2 activation and EGF-dependent DNA synthesis[2]. AG-494 significantly prevents NF-kB activation in silica-stimulated cells, and also reduces NF-kB activation in H2O2-treated cells[4]. AG-494 (3-9 μM; 5-7 days) inhibits BMP9-induced ALP activity in a dose-dependent manner[5].
References

[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]. Osherov N, et al. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997;410(2-3):187-190.

[3]. 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.

[4]. 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.

[5]. 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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 586.9±50.0 °C at 760 mmHg
Melting Point 249 °C(dec.)
Molecular Formula C16H12N2O3
Molecular Weight 280.278
Flash Point 308.8±30.1 °C
Exact Mass 280.084778
PSA 93.35000
LogP 2.40
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.736

 Safety Information

Hazard Codes C
Safety Phrases 22-24/25

 Synonyms

Tyrphostin 48
2-Propenamide, 2-cyano-3-(3,4-dihydroxyphenyl)-N-phenyl-, (2E)-
HMS3266B19
(2E)-2-Cyano-3-(3,4-dihydroxyphenyl)-N-phenylacrylamide
AG-494
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: AG-494
  • Price: $450.0/100mg $750.0/250mg $1500.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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Price: ¥1000/10 mg

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