Revision 4

#9842Store at -20C

 

Cell Signaling Technology

Orders: 877-616-CELL (2355) [email protected]

Support: 877-678-TECH (8324)

Web: [email protected] cellsignal.com

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For Research Use Only. Not for Use in Diagnostic Procedures.

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.

Molecular Formula

C16H14CIN3O2

Molecular Weight

315.76 g/mol

Purity

>99%

CAS

175178-82-2

Solubility

Soluble in DMSO at 10mg/ml.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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

    Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
    All other trademarks are the property of their respective owners. Visit cellsignal.com/trademarks for more information.

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    Revision 4
    #9842

    Tyrphostin AG 1478

    Tyrphostin AG 1478: Image 1 Expand Image
    Tyrphostin AG 1478 的结构
    Tyrphostin AG 1478: Image 2 Expand Image
    对未经处理或已经规定浓度的 Tyrphostin AG1478 处理 30 分钟,随后用 EGF 刺激 10 分钟的血清饥饿 A431 细胞的提取物进行蛋白质印迹分析。使用 Phospho-EGF Receptor (Tyr1173) (53A5) Rabbit mAb #4407(上图)可检测 EGFR 激活。EGF Receptor Antibody #2232 可用于检测 EGFR(下图)的相同上样量。Tyrphostin AG1478 介导的对 EGF 诱导的 EGF 受体 Tyr1173 磷酸化的抑制如图所示。