Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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B125789-5mg | 5mg | In stock | $58.90 | |
B125789-25mg | 25mg | In stock | $118.90 | |
B125789-100mg | 100mg | In stock | $177.90 | |
B125789-250mg | 250mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $400.90 | |
B125789-500mg | 500mg | In stock | $720.90 | |
B125789-1g | 1g | In stock | $1,297.90 |
Potent, selective, reversible\xa0proteasome inhibitor
Synonyms | CS-1039 | LDP 341 | BORTEZOMIB [MART.] | N-((1S)-1-benzyl-2-(((1R)-1-(dihydroxyboranyl)-3-methylbutyl)amino)2-oxoethylpyrazinecarboxamide | N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N(alpha)-(pyrazin-2-ylcarbonyl)-L-phenylalaninamide | N-[(1R)-1-(DIHYDR |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Bortezomib, a first-in-class proteasome inhibitor, induces apoptosis and growth arrest and reverses chemoresistance in myeloma cells and has demonstrated no irreversible adverse effect on haematopoietic stem cells. Bortezomib has shown in vitro and in viv |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | 26S proteosome inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM in a cell-free assay. |
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IUPAC Name | [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid |
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INCHI | 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 |
InChi Key | GXJABQQUPOEUTA-RDJZCZTQSA-N |
Canonical SMILES | B(C(CC(C)C)NC(=O)C(CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O |
Isomeric SMILES | B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O |
Alternate CAS | 1610526-91-4,179324-69-7 |
PubChem CID | 387447 |
NSC Number | 681239 |
MeSH Entry Terms | 341, PS;bortezomib;LDP 341;LDP-341;LDP341;PS 341;PS-341;PS341;Velcade |
Molecular Weight | 384.24 |
PubChem CID | 387447 |
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ChEMBL Ligand | CHEMBL325041 |
ChEBI | CHEBI:52717 |
CAS Registry No. | 179324-69-7 |
DrugBank Ligand | DB00188 |
Wikipedia | Bortezomib |
RCSB PDB Ligand | BO2 |
DrugCentral Ligand | 391 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
F2215351 | Certificate of Analysis | Mar 19, 2024 | B125789 |
F2215365 | Certificate of Analysis | Mar 19, 2024 | B125789 |
F2215366 | Certificate of Analysis | Mar 19, 2024 | B125789 |
F2215367 | Certificate of Analysis | Mar 19, 2024 | B125789 |
K21251140 | Certificate of Analysis | Sep 12, 2023 | B125789 |
K21251142 | Certificate of Analysis | Sep 12, 2023 | B125789 |
C1701090 | Certificate of Analysis | Sep 22, 2022 | B125789 |
G2307568 | Certificate of Analysis | Jun 01, 2022 | B125789 |
H2325036 | Certificate of Analysis | Jun 01, 2022 | B125789 |
L2314051 | Certificate of Analysis | Jun 01, 2022 | B125789 |
Solubility | Soluble in chloroform, dimethyl sulfoxide, ethanol and methanol;Soluble in water 76 mg/l |
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Sensitivity | light sensitive |
Refractive Index | 1.56 |
Boil Point(°C) | 684.30° C |
Melt Point(°C) | 139-143°C |
Pictogram(s) | GHS06, GHS08, GHS09, GHS07 |
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Signal | Danger |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H411:Toxic to aquatic life with long lasting effects H300:Fatal if swallowed H372:Causes damage to organs through prolonged or repeated exposure H361:Suspected of damaging fertility or the unborn child |
Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P362+P364:Take off contaminated clothing and wash it before reuse. P391:Collect spillage. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P318:if exposed or concerned, get medical advice. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
Merck Index | 1351 |
1. Jianhao Liu, Xiaoman Xu, Yanying Li, Jingxia Xu, Ruogang Zhao, Siwei Liu, Jingliang Wu, Li Zhang, Bo Zhang. (2023) Bortezomib-loaded mixed micelles realize a “three-in-one” effect for enhanced breast cancer treatment. Biomaterials Science, 11 (14): (4890-4906). [PMID:37306225] |
1. Reynolds JM, El Bissati K, Brandenburg J, Günzl A, Mamoun CB. (2007) Antimalarial activity of the anticancer and proteasome inhibitor bortezomib and its analog ZL3B.. BMC Clin Pharmacol, 7 (3): (13). [PMID:17956613] |
2. Ciechanover A. (2005) Intracellular protein degradation: from a vague idea, through the lysosome and the ubiquitin-proteasome system, and onto human diseases and drug targeting (Nobel lecture).. Angew Chem Int Ed Engl, 44 (37): (5944-67). [PMID:16142822] |
3. Groll M, Berkers CR, Ploegh HL, Ovaa H. (2006) Crystal structure of the boronic acid-based proteasome inhibitor bortezomib in complex with the yeast 20S proteasome.. Structure, 14 (3): (451-6). [PMID:16531229] |
4. Bonvini P, Zorzi E, Basso G, Rosolen A. (2007) Bortezomib-mediated 26S proteasome inhibition causes cell-cycle arrest and induces apoptosis in CD-30+ anaplastic large cell lymphoma.. Leukemia, 21 (4): (838-42). [PMID:17268529] |
5. Nakamura H, Watanabe M, Ban HS, Nabeyama W, Asai A. (2009) Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors.. Bioorg Med Chem Lett, 19 (12): (3220-4). [PMID:19428245] |
6. Zhang H, Liu Z, Huang L, Hou J, Zhou M, Huang X, Hu W, Liu Z. (2017) The short-term efficacy of bortezomib combined with glucocorticoids for the treatment of refractory lupus nephritis.. Lupus, 26 (9): (952-958). [PMID:28059023] |
7. Mazepa MA, Raval JS, Moll S, Ma A, Park YA. (2014) Bortezomib induces clinical remission and reduction of ADAMTS13 inhibitory antibodies in relapsed refractory idiopathic thrombotic thrombocytopenic purpura.. Br J Haematol, 164 (6): (900-2). [PMID:24345005] |
8. Wang Y, Zhou W, Zhang Z. (2015) Successful treatment of warm-type haemolytic anaemia with bortezomib in a rituximab-failed systemic lupus erythematosus patient.. Rheumatology (Oxford), 54 (1): (194-5). [PMID:25288787] |
9. Jakez-Ocampo J, Atisha-Fregoso Y, Llorente L. (2015) Refractory primary Sjögren syndrome successfully treated with bortezomib.. J Clin Rheumatol, 21 (1): (31-2). [PMID:25539431] |
10. Alexander T, Sarfert R, Klotsche J, Kühl AA, Rubbert-Roth A, Lorenz HM, Rech J, Hoyer BF, Cheng Q, Waka A et al.. (2015) The proteasome inhibitior bortezomib depletes plasma cells and ameliorates clinical manifestations of refractory systemic lupus erythematosus.. Ann Rheum Dis, 74 (7): (1474-8). [PMID:25710470] |
11. Xie SC, Gillett DL, Spillman NJ, Tsu C, Luth MR, Ottilie S, Duffy S, Gould AE, Hales P, Seager BA et al.. (2018) Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.. J Med Chem, 61 (22): (10053-10066). [PMID:30373366] |
12. Kao CC et al.. (2022) Mechanism of action of hepatitis B virus S antigen transport-inhibiting oligonucleotide polymer, STOPS, molecules.. Mol Ther Nucleic Acids, 27 (335-348). [PMID:35024245] |
13. Abdin SM et al.. (2021) Nuclear factor-?B signaling inhibitors revert multidrug-resistance in breast cancer cells.. Chem Biol Interact, 340 (109450). [PMID:33775688] |
14. Gain C et al.. (2020) Proteasomal inhibition triggers viral oncoprotein degradation via autophagy-lysosomal pathway.. PLoS Pathog, 16 (2): (e1008105). [PMID:32092124] |
15. Jianhao Liu, Xiaoman Xu, Yanying Li, Jingxia Xu, Ruogang Zhao, Siwei Liu, Jingliang Wu, Li Zhang, Bo Zhang. (2023) Bortezomib-loaded mixed micelles realize a “three-in-one” effect for enhanced breast cancer treatment. Biomaterials Science, 11 (14): (4890-4906). [PMID:37306225] |