Thalidomide, 5'-fluoro

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Description: Fluoro functionalized Thalidomide; cereblon ligand for PROTACs
Chemical Name: 2-(2,6-Dioxo-3-piperidinyl)-5-fluoro-1H-isoindole-1,3(2H)-dione
Purity: ≥95%
Literature (1)

Biological Activity for Thalidomide, 5'-fluoro

Thalidomide 5'- fluoro is a derivative of Thalidomide (Cat. No. 0652), commonly used as a precursor to PROTAC® Degraders that hijacks cereblon as the E3 ubiquitin ligase component. Supplied with a fluoro functional handle at a position known not to significantly affect binding to cereblon, ready for conjugation to a linker/target protein ligand.

Please contact us for SD files of our available Degrader Building Blocks.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Require a different derivative? Get in touch.

Usage Guidelines for Thalidomide, 5'-fluoro

This product is provided for use in onward chemistry. Suitable solvents can be used.

Technical Data for Thalidomide, 5'-fluoro

M. Wt 276.22
Formula C13H9FN2O4
Storage Store at +4°C
Purity ≥95%
CAS Number 835616-61-0
PubChem ID 70876201
Smiles FC1=CC=C2C(N(C(C2=C1)=O)C3CCC(NC3=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.

Product Datasheets for Thalidomide, 5'-fluoro

References for Thalidomide, 5'-fluoro

References are publications that support the biological activity of the product.

Burslem et al (2018) Efficient synthesis of immunomodulatory drug analogues enables exploration of structure-degradation relationships. Chem.Med.Chem. 13 1508 PMID: 29870139

If you know of a relevant reference for Thalidomide, 5'-fluoro, please let us know.

Keywords: Thalidomide, 5'-fluoro, Thalidomide, 5'-fluoro supplier, PROTACs, thalidomide, cereblon, E3, ligase, ligand, CRBN, fluoro, functionalized, Degrader, building, blocks, Functionalized, Ligase, Ligands, 7456, Tocris Bioscience

Citations for Thalidomide, 5'-fluoro

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Literature in this Area

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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