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Specifications
| Appearance | White to off-white solid |
| Purity | 99% min |
| Solubility | Soluble in dichloromethane and insoluble in cyclohexane |
| Keto Epoxide | 0.1% max |
| Main chain impurity | 0.5% max |
| Single impurity | 0.5% max |
| Water Content | 0.5% max |
Applications
1. Anticancer Drug – Proteasome Inhibitor
Carfilzomib is a second-generation proteasome inhibitor used as a targeted therapy for multiple myeloma, particularly in relapsed or refractory cases.
It selectively and irreversibly inhibits the chymotrypsin-like activity of the 20S proteasome, a key component of the ubiquitin-proteasome pathway responsible for protein degradation.
2. Treatment of Multiple Myeloma
Approved for patients who have received prior therapies, including bortezomib and immunomodulatory drugs.
Often used in combination with other drugs like lenalidomide and dexamethasone for enhanced therapeutic effect.
3. Research Tool
Utilized in biomedical research to study protein degradation, cellular apoptosis, and proteasome function.
Helps in understanding the role of proteasome inhibition in cancer and other diseases.
Benefits
✅ Potent and Selective Inhibitor
Irreversible binding ensures sustained inhibition of the proteasome activity.
✅ Reduced Toxicity Compared to First-Generation Inhibitors
Improved safety profile compared to bortezomib, with fewer off-target effects.
✅ Effective in Resistant Multiple Myeloma
Shows activity in patients refractory to other treatments.
✅ Intravenous Administration
Allows controlled dosing and bioavailability in clinical settings.
Conclusion
Carfilzomib (CAS 868540-17-4) is a highly potent and selective proteasome inhibitor revolutionizing treatment for multiple myeloma. Its irreversible mode of action and improved safety profile make it effective for patients resistant to earlier therapies. Beyond its clinical success, carfilzomib is a valuable research tool for probing proteasome biology and cancer cell apoptosis, underscoring its importance in both therapeutic and scientific contexts.
