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Gefitinib-based PROTAC® 3
Biological Activity for Gefitinib-based PROTAC® 3
Gefitinib-based PROTAC® 3 is a potent EGFR PROTAC® Degrader. Comprises an EGFR inhibitor gefitinib (Iressa Cat.No. 3000) conjugated to a VHL ligand via a linker. Induces EGFR degradation (DC50 values are 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively). Exhibits no degradation of wild-type EGFR at concentrations up to 10 μM.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for Gefitinib-based PROTAC® 3
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Gefitinib-based PROTAC® 3
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Gefitinib-based PROTAC® 3
The following data is based on the product molecular weight 934.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.07 mL||5.35 mL||10.7 mL|
|5 mM||0.21 mL||1.07 mL||2.14 mL|
|10 mM||0.11 mL||0.54 mL||1.07 mL|
|50 mM||0.02 mL||0.11 mL||0.21 mL|
Product Datasheets for Gefitinib-based PROTAC® 3
References for Gefitinib-based PROTAC® 3
References are publications that support the biological activity of the product.
Burslem et al (2018) The advantages of targeted protein degradation over inhibition: an RTK case study. Cell Chem.Biol. 25 67 PMID: 29129716
If you know of a relevant reference for Gefitinib-based PROTAC® 3, please let us know.
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Citations for Gefitinib-based PROTAC® 3
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Targeted Protein Degradation Research Product Guide
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia