Cell Signaling Technology

Product Pathways - Tyrosine Kinase / Adaptors

Tyrphostin AG 1478 #9842

Molecular Formula:
C16H14CIN3O2
Molecular Weight:
315.76 g/mol
Purity:
>99%

Directions for Use

Tyrphostin AG 1478 is supplied as 400 μg powder. Store at or below -20ºC. Before use, dissolve powder in 1.23 ml DMSO to make a 1 mM

Tyrphostin AG 1478 stock solution. For working concentrations of 100 nM-200 nM, dilute DMSO stock 1:10,000 to 1:5,000. Treat cells with the desired concentration for 30 minutes. Tyrphostin AG1478 is more stable as a powder than in solution; it is therefore recommended to dissolve as close as possible prior to use. Store solution at or below -20ºC.

Structure

Structure

Structure of Tyrphostin AG 1478

Western blot analysis of extracts from serum starved A431 cells, untreated or treated with indicated concentrations of Tyrphostin AG1478 for 30 minutes, followed by stimulation with EGF for 10 minutes. The EGFR activation was detected by using Phospho-EGF Receptor (Tyr1173) (53A5) Rabbit mAb #4407 (upper). EGF Receptor Antibody #2232 was used to detect the equal loading of EGFR (lower). Tyrphostin AG1478-mediated inhibition of EGF-induced phosphorylation of EGF Receptor at Tyr1173 is shown.

Background

Tyrphostin AG 1478 is a tyrosine kinase inhibitor specifically selective to EGFR (ErbB1), with an IC50 of about 3 nM in vitro (1,2). Treatment of cell with 50-150 nM of AG 1478 can substantially block EGFR activiation in vivo (3). In addition to EGFR, AG 1478 also inhibits ErbB4 activation induced by radiation in cancer cells (4). Testing of AG 1478 alone or in combination with other treatments to assess anti-tumor and anti-fibrotic effectiveness has yielded promising results (5-8).

  1. Osherov, N. and Levitzki, A. (1994) Eur J Biochem 225, 1047-53.
  2. Levitzki, A. and Gazit, A. (1995) Science 267, 1782-8.
  3. Fan, Z. et al. (1995) J Cell Biol 131, 235-42.
  4. Bowers, G. et al. (2001) Oncogene 20, 1388-97.
  5. Nagane, M. et al. (2001) J Neurosurg 95, 472-9.
  6. Ishii, Y. et al. (2006) Am J Respir Crit Care Med 174, 550-6.
  7. Ellis, A.G. et al. (2006) Biochem Pharmacol 71, 1422-34.
  8. Rahman, M. et al. (2009) Breast Cancer Res Treat 113, 217-30.

Application References

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Companion Products

For Research Use Only. Not For Use In Diagnostic Procedures.

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