All AbMole products are for research use only, cannot be used for human consumption.
Carfilzomib (PR-171) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. Carfilzomib irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme that degrades unwanted cellular proteins. Carfilzomib (PR-171) induced a dose- and time-dependent inhibition of proliferation, ultimately leading to apoptosis. Carfilzomib and its orally bioavailable analog oprozomib, effectively decreased MM cell viability following continual or transient treatment mimicking in vivo pharmacokinetics. In clinical trials, carfilzomib (PR-171) has exhibited potent anti-myeloma efficacy and decreased side effects compared with bortezomib. At clinically relevant concentrations, carfilzomib directly inhibited OC formation and bone resorption in vitro, while enhancing osteogenic differentiation and matrix mineralization. Carfilzomib is currently in a phase III confirmatory clinical trial, known as the ASPIRE trial, comparing carfilzomib, lenalidomide and dexamethasone versus lenalidomide and dexamethasone in patients with relapsed multiple myeloma.Carfilzomib showed stronger inhibitory activity and longer inhibition time against bortezomib resistant cells, and showed higher selectivity against proteasome. Its IC50 against 20S proteasome β5 was 3.4nmol/L.
*The compound is unstable in solutions, freshly prepared is recommended.
| Molecular Weight | 719.91 |
| Formula | C40H57N5O7 |
| CAS Number | 868540-17-4 |
| Solubility (25°C) | DMSO 65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Proteasome Products |
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| IU1
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