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Bortezomib (PS-341)

In stock
Catalog No.
A2614
Proteasome Inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
Evaluation Sample
$28.00
In stock
10mg
$60.00
In stock
25mg
$108.00
In stock
100mg
$250.00
In stock
500mg
$680.00
In stock

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Background

Bortezomib (originally codenamed PS-341) is the first therapeutic proteasome inhibitor to the tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. [1] The drug is an N-protected dipeptide and can be written as Pyz-Phe-boroLeu, which stands for pyrazinoic acid, phenylalanine and Leucine with a boronic acid instead of a carboxylic acid. Peptides are written N-terminus to C-terminus, and this convention is used here even though the "C-terminus" is a boronic acid instead of a carboxylic acid. While multiple mechanisms are likely to be involved, proteasome inhibition may prevent degradation of pro-apoptotic factors, permitting activation of programmed cell death in neoplastic cells dependent upon suppression of pro-apoptotic pathways. Recently, it was found that bortezomib caused a rapid and dramatic change in the levels of intracellular peptides that are produced by the proteasome. [2] Some intracellular peptides have been shown to be biologically active, and so the effect of bortezomib on the levels of intracellular peptides may contribute to the biological and/or side effects of the drug.

A potent (Ki = 0.6 nM), specific and reversible proteasome inhibitor. It inhibits cell proliferation of H460 cells (Human non-small cell lung cancer cell lines) with an IC₅₀ of 0.1 µM.

References:
1. Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.
2. Gelman JS, Sironi J, Berezniuk I, Dasgupta S, Castro LM, Gozzo FC, Ferro ES, Fricker LD (2013). "Alterations of the intracellular peptidome in response to the proteasome inhibitor bortezomib". In Gartel, Andrei L. PLoS One 8 (8): e53263.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt384.24
Cas No.179324-69-7
FormulaC19H25BN4O4
SynonymsBortezomib,PS-341,LDP-341,MLM341,MG-341,NSC-681239
Solubility≥19.212mg/mL in DMSO
Chemical Name[(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
SDFDownload SDF
Canonical SMILESB(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

Canine malignant melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

72h; IC50=3.5~5.6 nM (nine kinds of cells)

Applications

Bortezomib potently suppressed the growth in 21 drugs, while other compounds had no or minimal effect on cell growth. We thus focused on bortezomib and examined its growth inhibitory properties against nine canine malignant melanoma cell lines (CMM-1, CMM-2, ChMC, KMeC, LMeC, OMJ, OMS, OMK, and NML). Bortezomib inhibited the growth of all cell lines with calculated IC50 values of 3.5~5.6 nM.

Animal experiment [1]:

Animal models

Nude athymic mice

Dosage form

0.8 mg/kg; intravenous injection

Applications

The in vivo growth inhibitory activity of bortezomib against CMM-1 cells was evaluated using a xenograft mouse model. Bortezomib significantly suppressed the growth of tumours after Day 4 of treatment (P < 0.01, control vs. bortezomib). Tumours from the bortezomib-treated mice showed a significant decrease in mitotic index compared to controls (P<0.01). Similarly, the Ki67 index was significantly decreased in tumours excised from the bortezomib-treated mice when compared to controls (P < 0.01).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Ito K, Kobayashi M, Kuroki S, et al. The proteasome inhibitor bortezomib inhibits the growth of canine malignant melanoma cells in vitro and in vivo[J]. The Veterinary Journal, 2013, 198(3): 577-582.

Biological Activity

Description Bortezomib (PS-341) is a potent inhibitor of 20S proteasome with Ki of 0.6 nM.
Targets 20S proteasome          
IC50 0.6 nM (Ki)          

Quality Control

Chemical structure

PS341

Related Biological Data

PS341

Related Biological Data

PS341

Related Biological Data

PS341

Related Biological Data

PS341

Related Biological Data

PS341

Related Biological Data

PS341

Related Biological Data

PS341