Cell Signaling Technology

Product Pathways - Tyrosine Kinase / Adaptors

Erlotinib #5083

Molecular Formula:
C22H23N3O4
Molecular Weight:
429.90 g/mol
Purity:
>99%

Directions for Use

Erlotinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 2.54 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-2 hours prior to treating with a stimulator. It can also be used alone, with varying treatment times lasting up to 24 hours. Soluble in DMSO at 100 mg/ml, soluble in ethanol at 10 mg/ml with warming; very poorly soluble in water with a maximum solubility ~5-20 µM.

Western Blotting

Western Blotting

Western blot analysis of extracts from A-431 cells, serum-starved overnight and untreated or treated with hEGF #8916 (100 ng/ml, 5 min) either with or without Erlotinib pre-treatment (1 hr) at the indicated concentrations, using Phospho-EGF Receptor (Tyr1068) (D7A5) XP® Rabbit mAb #3777 (upper) or EGF Receptor (D38B1) XP® Rabbit mAb #4267 (lower).

Structure

Structure

Chemical structure of Erlotinib.

Background

Erlotinib is a novel and potent ATP-competitive inhibitor of the EGFR kinase pathway. It inhibited EGFR autophosphorylation with an IC50 of 20 nM in vitro and inhibit purified EGFR kinase with an IC50 of 2 nM (1). Erlotonib is greater than 1000-fold more selective for EGFR than c-src and v-abl (1), ErbB-2, and ErbB-4 (2). Studies have shown that erlotinib inhibits growth and induces G1 cell cycle arrest in multiple cell types, many of which overexpress EGFR (1,3-5).

  1. Moyer, J.D. et al. (1997) Cancer Res 57, 4838-48.
  2. Wood, E.R. et al. (2004) Cancer Res 64, 6652-9.
  3. Huether, A. et al. (2005) J Hepatol 43, 661-9.
  4. Ling, Y.H. et al. (2007) Mol Pharmacol 72, 248-58.
  5. Yamasaki, F. et al. (2007) Mol Cancer Ther 6, 2168-77.

Application References

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

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