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Submit ReviewCarfilzomib
Description: Potent irreversible proteasome inhibitor; active in vivo
Alternative Names: PR-171
Chemical Name: (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide
Purity: ≥98% (HPLC)
Biological Activity for Carfilzomib
Carfilzomib is a potent irreversible proteasome inhibitor. Preferentially inhibits the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM) in vitro with minimal cross-reactivity to other proteases. Exhibits little or no effect on PGPH and T-L activities. Activates prosurvival autophagy and induces cell apoptosis. Acts synergistically with dexamethasone (Cat. No. 1126). Suppresses tumor growth in an in vivo xenograft model. Decreases bone resorption and enhances bone formation in non-tumor bearing mice.
Technical Data for Carfilzomib
| M. Wt | 719.92 |
| Formula | C40H57N5O7 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 868540-17-4 |
| PubChem ID | 11556711 |
| InChI Key | BLMPQMFVWMYDKT-NZTKNTHTSA-N |
| Smiles | CC(C)C[C@H](NC(=O)[C@H](CCC1=CC=CC=C1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1 |
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 Carfilzomib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 71.99 | 100 | |
| ethanol | 14.4 | 20 |
Preparing Stock Solutions for Carfilzomib
The following data is based on the product molecular weight 719.92. 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 | 1.39 mL | 6.95 mL | 13.89 mL |
| 5 mM | 0.28 mL | 1.39 mL | 2.78 mL |
| 10 mM | 0.14 mL | 0.69 mL | 1.39 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.28 mL |
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Product Datasheets for Carfilzomib
References for Carfilzomib
References are publications that support the biological activity of the product.
Demo et al (2007) Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. Cancer Res. 67 6383 PMID: 17616698
Zhou et al (2009) Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J.Med.Chem. 52 3028 PMID: 19348473
Dou et al (2014) Overview of proteasome inhibitor-based anti-cancer therapies: perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system. Curr.Cancer Drug Targets 14 517 PMID: 25092212
Wang et al (2020) Fast identification of possible drug treatment of coronavirus disease-19 (COVID-19) through computational drug repurposing study. J.Chem.Inf.Model 60 3277 PMID: 32315171
If you know of a relevant reference for Carfilzomib, please let us know.
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Keywords: Carfilzomib, Carfilzomib supplier, Potent, irreversible, proteasome, inhibitor, inhibitors, inhibits, inhibit, active, in, vivo, 20S, proteasomes, 20Si, PR-171, Proteasome, 7188, Tocris Bioscience
Citations for Carfilzomib
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Reviews for Carfilzomib
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Apoptosis induction.
By
MARINA KOUTSIOUMPA on 10/13/2022
Assay Type: In Vitro
Species: Human
Combinatorial treatments of carfilzomib with chemotherapeutics led to synergistic apoptotic phenotype in vitro.
Literature in this Area
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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
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