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Biological Activity for Bortezomib
Bortezomib is a high affinity proteasome inhibitor (Ki = 0.6 nM). Inhibits growth of multiple myeloma (MM) cell lines (IC50 values in <50 nM range); induces apoptosis in MM cell lines and MM patient derived cells, including p53 mutant cell lines. Decreases adherence of MM cells lines to bone marrow stromal cells (BMSCs). Acts synergistically with dexamethasone (Cat. No. 1126). Also cytotoxic in MCF-7 breast cancer cell line (IC50 = 50 nM).
Technical Data for Bortezomib
|Storage||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.
Solubility Data for Bortezomib
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Bortezomib
The following data is based on the product molecular weight 384.24. 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|
|1.31 mM||1.99 mL||9.93 mL||19.87 mL|
|6.55 mM||0.4 mL||1.99 mL||3.97 mL|
|13.1 mM||0.2 mL||0.99 mL||1.99 mL|
|65.5 mM||0.04 mL||0.2 mL||0.4 mL|
References for Bortezomib
References are publications that support the biological activity of the product.
Teicher et al (1999) The proteasome inhibitor PS-341 in cancer therapy. Clin.Cancer Res. 5 2638 PMID: 10499643
Hideshima et al (2001) The proteasome inhibitor PS-341 inhibits growth, induces apoptosis, and overcomes drug resistance in human multiple myeloma cells. Cancer Res. 61 3071 PMID: 11306489
If you know of a relevant reference for Bortezomib, please let us know.
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Keywords: Bortezomib, Bortezomib supplier, PS341, proteasome, inhibitor, multiple, myeloma, high, affinity, Proteasome, 7282, Tocris Bioscience
Citations for Bortezomib
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Literature in this Area
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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
- Degrader Building Blocks
- Custom Degrader Services
- UPS Proteins and Assays
- Assays for Protein Degradation
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