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).
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- Levitzki, A. and Gazit, A. (1995) Science 267, 1782-8.
- Fan, Z. et al. (1995) J Cell Biol 131, 235-42.
- Bowers, G. et al. (2001) Oncogene 20, 1388-97.
- Nagane, M. et al. (2001) J Neurosurg 95, 472-9.
- Ishii, Y. et al. (2006) Am J Respir Crit Care Med 174, 550-6.
- Ellis, A.G. et al. (2006) Biochem Pharmacol 71, 1422-34.
- Rahman, M. et al. (2009) Breast Cancer Res Treat 113, 217-30.
Molecular Formula
C16H14CIN3O2
Molecular Weight
315.76 g/mol
Purity
>99%
CAS
175178-82-2
Solubility
Soluble in DMSO at 10mg/ml.
Storage
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.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
Limited Uses
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