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PS-341 (Bortezomib) | Proteasome inhibitor

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Price:
$89.00
Catalog #:
C7734-5
Quantity:


Product Description

Bortezomib is a first-in-class dipeptide boronic acid-based, water-soluble proteasome inhibitor. As a single agent, bortezomib was found to have consistent antitumor activity in both chemosensitive and chemoresistant multiple myeloma cells at an IC50 of 10-20 ng/mL. [1] Bortezomib overcomes the resistance to apoptosis in multiple myeloma cells that is induced by IL-6. [2] Additionally, bortezomib prevents TNF-a-induced, NF-kB-dependent upregulation of IL-6 and reduces cell adhesion; proliferation of remaining adherent multiple myeloma cells was also inhibited by bortezomib. [1]

In MM cell lines U266, IM-9, and Hs Sultan, bortezomib inhibited at IC50 concentrations of 3, 6, and 20 nM, respectively. [2] Cell growth of Dox40, MR20, and LR5 MM cells was completely inhibited by bortezomib at 100 nM IC50.

Bortezomib suppresses growth and induces apoptosis in Bcr/Abl-positive cells sensitive and resistant to IM. Interestingly, sequential combination of bortezomib followed by imatinib resulted in a synergistic pro-apoptotic effect in imatinib-resistant cells; simultaneous exposure of bortezomib and imatinib was antagonistic. [3]


Technical information:

Chemical Formula:   C19H25BN4O4
CAS #:   179324-69-7
Molecular Weight:   384.24
Purity:   >98%
Appearance:   Light Yellow Crystalline
Chemical Name:   [(1R)-3-methyl-1-({(2S)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl}amino)butyl]boronic acid
Solubility:   Up to 100 mM in DMSO
Synonyms:   PS-341, PS341, Bortezomib, Velcade, LDP-341

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Richardson et al., Cancer Control, 2003, 10(6), 361-369.
2. Hideshima et al., The proteasome inhibitor PS-341 inhibits growth, induces apoptosis, and overcomes drug resistance in human multiple myeloma cells. Cancer Res. 2001, 61, 3071-3076. Pubmed ID: 1306489
3. Gatto et al., The proteasome inhibitor PS-341 inhibits growth and induces apoptosis in Bcr/Abl-positive cell lines sensitive and resistant to imatinib mesylate. Haematologica, 2003, 88(8), 853-863. Pubmed ID: 12935973

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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