Gefitinib-based PROTAC® 3

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Description: Potent EGFR PROTAC®
Alternative Names: Iressa-based PROTAC 3
Chemical Name: (2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Literature (4)

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

M. Wt 934.52
Formula C47H57ClFN7O8S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2230821-27-7
PubChem ID 135156947
Smiles COC1=CC2=C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)C=C1OCCCCCOCCOCCC(N[C@@H](C(C)(C)C)C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)O)=O)=O

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
DMSO 93.45 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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

Citations are publications that use Tocris products.

Currently there are no citations for Gefitinib-based PROTAC® 3. Do you know of a great paper that uses Gefitinib-based PROTAC® 3 from Tocris? Please let us know.

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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

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

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

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

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