Carfilzomib

Biological Activity

Carfilzomib is a potent irreversible proteasome inhibitor. Preferentially inhibits 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) in vitro with minimal cross-reactivity to other proteases. Exhibits little or no effect on PGPH and T-L activities. Activates prosurvival autophagy and induces cell apoptosis. Acts synergistically with dexamethasone (Cat. No. 1126). Suppresses tumor growth in an in vivo xenograft model. Decreases bone resorption and enhances bone formation in non-tumor bearing mice.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome.
   Demo et al.
   Cancer Res., 2007;67:6383
2. Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).
   Zhou et al.
   J.Med.Chem., 2009;52:3028
3. Overview of proteasome inhibitor-based anti-cancer therapies: perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system.
   Dou et al.
   Curr.Cancer Drug Targets, 2014;14:517
4. Fast identification of possible drug treatment of coronavirus disease-19 (COVID-19) through computational drug repurposing study.
   Wang et al.
   J.Chem.Inf.Model, 2020;60:3277

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