Carfilzomib [PR-171]

Synthetic. Chemical. CAS: 868540-17-4. Formula: C40H57N5O7. MW: 719.9. Synthetic. Potent and irreversible second-generation peptide epoxyketone class proteasome inhibitor. Synthetic analog of the microbial product epoxomcin. Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=5.2nM) and the beta5i subunit [LMP7] of the 20S immunoproteasome (IC50=14nM), with minimal crossreactivity to other proteases. Displays equal potency but greater selectivity for the chymotrypsin-like activity of the proteasome compared to bortezomib. Anticancer compound effective against multiple myeloma in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma, and various solid tumors (IC50s=2.4-20nM).