SML4493

Carfilzomib

≥98% (HPLC)

• Synonym(e): (aS)-a-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide, PR 171, PR-171
• Empirische Formel (Hill-System): C₄₀H₅₇N₅O₇
• CAS-Nummer: 868540-17-4
• Molekulargewicht: 719.91
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: (Powder or Lyophilized powder or Film)

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: (Powder or Lyophilized powder or Film)
• color: white to off-white
• storage temp.: -10 to -25°C

Beschreibung

Biochem/physiol Actions

Carfilzomib (PR-171) is a definitive, cell-permeable, irreversible tetrapeptide epoxyketone proteasome inhibitor that selectively targets the chymotrypsin-like (ChT-L) activity of the constitutive 20S proteasome (β5) and immunoproteasome (LMP7/β5i) with nanomolar potency (IC50 < 5 nM). By forming specific morpholino adducts with catalytic N-terminal threonines, PR-171 decouples pharmacokinetics from pharmacodynamics, ensuring sustained target suppression despite rapid systemic clearance (t1/2 < 30 min). Unlike boronic acid predecessors, the epoxyketone exhibits negligible affinity for non-proteasomal serine proteases (e.g., cathepsin G, elastase), resulting in a superior neurotoxicity profile. Mechanistically, Carfilzomib blocks NF-κB signaling via IκBα stabilization and drives the accumulation of poly-ubiquitinated proteins, precipitating catastrophic ER stress, mitochondrial depolarization, and JNK-mediated apoptosis. Clinically validated for relapsed/refractory multiple myeloma, PR-171 overcomes bortezomib resistance and demonstrates profound synergy with dexamethasone, lenalidomide and daratumumab in high-risk phenotypes.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable