Carfilzomib, Free Base (Kyprolis, PR-171, CAS 868540-17-4), >99%

LC Laboratories' Product Number C-3022 - Carfilzomib, Free Base (Kyprolis, PR-171, CAS 868540-17-4), >99% - for research use only. Carfilzomib, also known as PR-171, is an irreversible, epoxomicin-related proteasome inhibitor. It potently bound to and specifically inhibited the chymotrypsin-like proteasome (ChT-L) and immunoproteasome activities in the β5 subunit with >80% inhibition at doses of ≥10 nM. It showed little or no effect on the postglutamyl peptide hydrolyzing (PGPH) activity in the β1 subunit and trypsin-like (T-L) activity in the β2 subunit at doses of ≤100 nM in vitro. It also inhibited the proliferation of IL-6-independent and -dependent myeloma cell lines with an IC50 of <5 nM in both and ultimately led to apoptosis. Carfilzomib demonstrated higher efficacy compared with bortezomib (please see Cat. No. B-1408, Bortezomib, Free Base) and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Furthermore, carfilzomib overcame resistance to other conventional agents. Coadministration of carfilzomib with the histone deacetylase inhibitor vorinostat (please see Cat. No. V-8477, Vorinostat) resulted in sharp increases in mitochondrial injury and apoptosis in multiple mantle cell lymphoma (MCL) cell lines and primary MCL cells. Carfilzomib/vorinostat coadministration also induced a pronounced reduction in tumor growth compared with single agent treatment in an MCL xenograft model. The response data for single-agent carfilzomib were very promising in bortezomib-naive patients with relapsed and/or refractory multiple myeloma in a phase 2 clinical trial. Carfilzomib is the active ingredient in the drug product sold under the trade name Kyprolis®. This drug is currently approved in at least one country for use in patients with multiple myeloma. NOTE: THE CARFILZOMIB RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT KYPROLIS®, AND IS NOT FOR HUMAN USE.

• Supplier: LC Laboratories
• Product #: C-3022
• Sku #: C-3022_1g