Gefitinib-based PROTAC® 3

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Gefitinib-based PROTAC® 3 | CAS No. 2230821-27-7 | Active Degraders
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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%

Product Details

Biological Activity

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

Soluble to 100 mM in DMSO
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.

Background References

  1. The advantages of targeted protein degradation over inhibition: an RTK case study.
    Burslem et al.
    Cell Chem.Biol., 2018;25:67

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