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5083
Erlotinib
Activators & Inhibitors
Chemical Modulators

Erlotinib #5083

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Erlotinib: Image 1

Chemical structure of Erlotinib.

Erlotinib: Image 2

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).

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 393.44 g/mol
Purity

>99%

Molecular Formula

C22H23N3O4

CAS 183321-74-6
Solubility Soluble in DMSO at 100mg/ml and EtOH at 10mg/ml.

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).

This product has applications to SARS-CoV-2 research into the mechanisms of the Novel Coronavirus, which has caused the COVID-19 pandemic.

  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.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
To Purchase # 5083S
Product # Size Price
5083S
10 mg N/A

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