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Biological Activity for Pomalidomide
Pomalidomide is a potent TNF-α inhibitor (IC50 = 13 nM). Also potently inhibits IL-2 (EC50 = 8 nM). Thalidomide derivative. Binds cereblon and inhibits its ubiquitination. Exhibits antiproliferative effects in a Namalwa lymphoma cell line. Antiangiogenic. Promotes degradation of transcription factor SALL4.
Technical Data for Pomalidomide
|Storage||Store at +4°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 Pomalidomide
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Pomalidomide
The following data is based on the product molecular weight 273.24. 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||3.66 mL||18.3 mL||36.6 mL|
|5 mM||0.73 mL||3.66 mL||7.32 mL|
|10 mM||0.37 mL||1.83 mL||3.66 mL|
|50 mM||0.07 mL||0.37 mL||0.73 mL|
References for Pomalidomide
References are publications that support the biological activity of the product.
Lohbeck & Miller (2016) Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development. Bioorg.Med.Chem.Lett. 26 5260 PMID: 27687673
Nanthakumar et al (2015) Dissecting fibrosis: therapeutic insights from the small-molecule toolbox. Nat.Rev.Drug.Discov. 14 693 PMID: 26338155
Lai et al (2016) Modular PROTAC design for the degradation of oncogenic BCR-ABL. Angew.Chem.Int.Ed.Engl. 55 807 PMID: 26593377
Winter et al (2015) Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 348 1376 PMID: 25999370
Donovan et al (2018) Thal. promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray Syndrome. Elife 7 e38430 PMID: 30067223
Chamberlain et al (2019) Evolution of cereblon-mediated protein degradation as a therapeutic modality. ACS Med.Chem.Lett. 10 1592 PMID: 31857833
If you know of a relevant reference for Pomalidomide, please let us know.
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Citations for Pomalidomide
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Literature in this Area
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Targeted Protein Degradation Research Product Guide
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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