News from the Bench

Discover what’s going on at CST, receive our latest application notes and tips, read our science features, and learn about our products.

Subscribe

Our U.S. Offices Are Closed

Our U.S. offices are closed in observance of the holidays. We will reopen on Monday, December 29th.

Thank you for your patience.

To Purchase # 5083S

5083S 10 mg

To get local purchase information on this product, click here

Questions?

Find answers on our FAQs page.

ANSWERS  

Visit PhosphoSitePlus®

PTM information and tools available.

LEARN MORE

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).

Learn more about how we get our images

Chemical structure of Erlotinib.

Learn more about how we get our images
Image

Product Usage Information

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.


Storage: Store lyophilized or in solution at -20ºC, desiccated. 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.

Product Description

Molecular Weight:

429.90 g/mol


Purity:

>99%


Molecular Formula:

C22H23N3O4


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.



For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology® is a trademark of Cell Signaling Technology, Inc.