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Submit ReviewPomalidomide
Description: Cereblon binder; also TNF-α inhibitor and antiangiogenic
Chemical Name: 4-Amino-2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione
Purity: ≥98% (HPLC)
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
| M. Wt | 273.24 |
| Formula | C13H11N3O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 19171-19-8 |
| PubChem ID | 134780 |
| InChI Key | UVSMNLNDYGZFPF-UHFFFAOYSA-N |
| Smiles | NC1=CC=CC2=C1C(N(C2=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.
Solubility Data for Pomalidomide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.32 | 100 |
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 |
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Product Datasheets for Pomalidomide
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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Keywords: Pomalidomide, Pomalidomide supplier, Pomalidomide, TNFa, TNFalpha, TNFα, Inhibitors, inhibits, IL-2, thalidomide, cereblon, binder, ubiquitination, antiproliferative, antiangiogenic, lymphoma, SALL4, CELMoD, E3, ligase, modulators, immunomodulators, immunomodulatory, imide, IMiDs, Ubiquitin, Ligases, Cytokines, Antiangiogenics, Other, Transcription, Factors, Molecular, Glues, 6302, Tocris Bioscience
1 Citation for Pomalidomide
Citations are publications that use Tocris products. Selected citations for Pomalidomide include:
Francisca et al (2022) Systematic profiling of conditional degron tag technologies for target validation studies. Nat Commun 13 5495 PMID: 36127368
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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!
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TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
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