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Purity: ≥98%
Bortezomib (formerly also known as PS-341; trade name Velcade among others), a dipeptide boronic acid derivative, is cell-permeable, reversible, potent and highly selective inhibitor of the 20S proteasome that may have antitumor effects. In a test without cells, it inhibits the 20S proteasome with a Ki of 0.6 nM. The controlled breakdown of proteins involved in cell cycle regulation and tumor growth is facilitated by the ubiquitin-proteasome pathway. Tumor growth should be significantly impacted and cell death should result from dysregulating the degradation of these proteins. Bortezomib was licensed in 2003 in the United States and Europe for the treatment of relapsed multiple myeloma and mantle cell lymphoma. It is a potent 20S proteasome inhibitor with potential antineoplastic activity. A big protease complex called the 26S proteasome breaks down ubiquinated proteins; benetezomib reversibly inhibits this complex. Bortezomib amplifies the cytotoxic effects of chemotherapy and radiation while delaying the growth of tumors in vivo.
| Targets |
NF-κB; 20S proteasome (Ki = 0.6 nM)
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|---|---|
| ln Vitro |
is a highly selective, reversible inhibitor of the 26S proteasome, which is mainly involved in the breakdown of misfolded proteins and is crucial for controlling the cell cycle. It is a boronic acid dipeptide. It has been demonstrated that exposure to boratezomib stabilizes p21, p27, and p53 in addition to the proapoptotic Bax and Bid proteins, caveolin-1, and inhibitor κB-α, which stops nuclear factor κB-induced cell survival pathways from activating. Additionally, boratezomib stimulates the endoplasmic reticulum stress response and proapoptotic c-Jun-NH2 terminal kinase. Changes in these cellular protein levels cause cancer cells to proliferate less, migrate less, and undergo apoptosis more frequently.[2] It has been demonstrated that boratezomib can enter cells and block the intracellular proteolysis of long-lived proteins by proteasomes at a concentration that can stop 50% of the proteolysis at about 0.1 μM. Throughout the panel of 60 cancer cell lines obtained from various human tumors from the US National Cancer Institute (NCI), the average growth inhibition of 50% value for Bortezomib is 7 nM. Bortezomib (100 nM) treatment of PC-3 cells for 8 hours causes a decrease in G1 cell count and an increase in G2-M cell accumulation. PC-3 cells are killed by benetezomib at 24 and 48 hours, with IC50 values of 100 and 20 nM, respectively. Nuclear condensation is brought on by benezomib 16–24 hours after treatment. In a time-dependent manner, benezomib treatment causes PARP cleavage; at 24 hours, concentrations as low as 100 nM are effective.[1]
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| ln Vivo |
In xenograft models of multiple myeloma, adult T-cell leukemia, lung, breast, prostate, pancreatic, head and neck, and colon cancer, as well as melanoma, the anticancer effects of bortezomib as a single agent have been shown.[2] In the Lewis lung cancer model, oral bortezomib 1.0 mg/kg daily for 18 days results in tumor growth delays and a reduction in the number of metastases. A single dose of up to 5 mg/kg of borectezomib markedly reduced the percentage of breast tumor cells that survived. Takedaskomib When given weekly for four weeks, 1.0 mg/kg of prostate cancer reduces tumor growth in murine xenograft models by 60%. When administered at a dose of 1.0 mg/kg for four weeks, pancreatic cancer murine xenografts grow 72% or 84% less, and tumor cell apoptosis rises. Treatment with 1.0 mg/kg Bortezomib causes a notable reduction in the growth of human plasmacytoma xenografts, an increase in the apoptosis and overall survival of tumor cells, and a decrease in tumor angiogenesis. [3]
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| Enzyme Assay |
Suc-Leu-Leu-Val-Tyr-AMC in DMSO and 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) are added to a 3 mL fluorescence cuvette in a typical kinetic run. The cuvette is then placed in the jacketed cell holder of a fluorescence spectrophotometer. A water bath that circulates keeps the reaction temperature at 37°C. One microliter to ten microliters of the stock enzyme solution are added to the cuvette once the reaction solution has reached thermal equilibrium, which takes five minutes. The degree of fluorescence emission that increases at 440 nm (λex= 380 nm) when AMC is cleaved from peptide-AMC substrates indicates the progress of the reaction.
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| Cell Assay |
The MTT dye absorbance of the cells is used to measure the inhibitory effect of boratezamib on cell growth. For the final four hours of the 48-hour cultures, cells are pulsed with 10 μL of 5 mg/mL MTT in each well. This is followed by 100 μL of isopropanol containing 0.04 N HCl. The absorbance is determined with a spectrophotometer at 570 nm.
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| Animal Protocol |
Human plasmacytoma xenografts RPMI 8226
1 mg/kg i.v. twice weekly for 4 weeks, then once weekly |
| References |
| Molecular Formula |
C19H25BN4O4
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|---|---|
| Molecular Weight |
384.24
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| Exact Mass |
384.20
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| Elemental Analysis |
C, 59.39; H, 6.56; B, 2.81; N, 14.58; O, 16.66
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| CAS # |
179324-69-7
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| Related CAS # |
Bortezomib-d8
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| Appearance |
white solid powder
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| SMILES |
B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
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| InChi Key |
GXJABQQUPOEUTA-RDJZCZTQSA-N
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| InChi Code |
InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1
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| Chemical Name |
[(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
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| Synonyms |
NSC 681239; PS-341; PS341; MLN-341; PS 341; LDP-341; LDP 341; LDP341; MLN341; MLN 341. Brand name: VELCADE
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6025 mL | 13.0127 mL | 26.0254 mL | |
| 5 mM | 0.5205 mL | 2.6025 mL | 5.2051 mL | |
| 10 mM | 0.2603 mL | 1.3013 mL | 2.6025 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05805891 | Recruiting | Drug: bortezomib | Rheumatoid Arthritis | Chinese SLE Treatment And Research Group |
June 2025 | Not Applicable |
| NCT05383547 | Recruiting | Drug: bortezomib | Bortezomib MN |
Ruijin Hospital | August 2, 2022 | Not Applicable |
| NCT03737136 | Recruiting | Drug: bortezomib | Antibody-mediated Rejection | Shahid Beheshti University of Medical Sciences |
November 1, 2019 | Not Applicable |
| NCT01453088 | Active Recruiting |
Drug: Melphalan Drug: Bortezomib |
Multiple Myeloma | Hackensack Meridian Health | June 24, 2010 | Phase 2 |
| NCT02139397 | Active Recruiting |
Drug: DFMO Drug: Bortezomib |
Neuroblastoma Recurrent | Giselle Sholler | May 2014 | Phase 1 Phase 2 |
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