2319881-95-1

Carfilzomib impurity 13 (hydrochloride) is a potential impurity found in commercial carfilzomib preparations. Carfilzomib (Item No. 17554) is a second-generation, irreversible, peptide epoxyketone class proteasome inhibitor that targets the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM) with minimal cross reactivity to other proteases.1,2 It can induce cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma, and various solid tumors (IC50s = 2.4-20 nM).3WARNING This product is not for human or veterinary use.

[1] Q PING DOU J A Z. Overview of proteasome inhibitor-based anti-cancer therapies: perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system.[J]. Current cancer drug targets, 2014, 14 6: 517-536. DOI: 10.2174/1568009614666140804154511
[2] HAN-JIE ZHOU*. Design and Synthesis of an Orally Bioavailable and Selective Peptide Epoxyketone Proteasome Inhibitor (PR-047)[J]. Journal of Medicinal Chemistry, 2009, 52 9: 3028-3038. DOI: 10.1021/jm801329v
[3] SUSAN D DEMO. Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome.[J]. Cancer research, 2007, 67 13: 6383-6391. DOI: 10.1158/0008-5472.can-06-4086