Bortezomib

Biological Activity

Bortezomib is a high affinity proteasome inhibitor (K_i = 0.6 nM). Inhibits growth of multiple myeloma (MM) cell lines (IC₅₀ values in <50 nM range); induces apoptosis in MM cell lines and MM patient derived cells, including p53 mutant cell lines. Decreases adherence of MM cells lines to bone marrow stromal cells (BMSCs). Acts synergistically with dexamethasone (Cat. No. 1126). Also cytotoxic in MCF-7 breast cancer cell line (IC₅₀ = 50 nM).

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. The proteasome inhibitor PS-341 in cancer therapy.
   Teicher et al.
   Clin.Cancer Res., 1999;5:2638
2. The proteasome inhibitor PS-341 inhibits growth, induces apoptosis, and overcomes drug resistance in human multiple myeloma cells.
   Hideshima et al.
   Cancer Res., 2001;61:3071

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