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504314 Bortezomib - CAS 179324-69-7 - Calbiochem

Bortezomib, CAS 179324-69-7, is a cell-permeable, selective, slowly reversible inhibitor of 20S proteasome β5 ChTL/chymotrypsin- over β1 CL/caspase- and β2 TL/trypsin-like activity.

Bortezomib - CAS 179324-69-7 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: BTZ, LDP-341, LDP341, MG341, MLN-341, MLN341, PS341, Proteasome Inhibitor XXII, PS-341, MG-341, Pyz-Phe-boroLeu, (R)-3-Methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butylboronic acid

Primary Target: 20S proteasome
504314
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
179324-69-7C₁₉H₂₅BN₄O₄

Products

RéférenceConditionnement Qté
5043140001 Flacon en verre 5 mg
Description
OverviewA cell-permeable dipeptidylboronate compound that selectively inhibits 20S proteasome β5 ChTL/chymotrypsin- over β1 CL/caspase- and β2 TL/trypsin-like activity (kinact/Ki = 38,000, 5,700, and <100 M-1s-1, respectively, in human 20S proteasome assays using 10 µM Suc-LLVY-AMC/Cat. No. 539142, 10 µM Z-LLE-AMC/Cat. No. 539141, or 50 µM Boc-LRR-AMC as substrate) via a covalent, slowly reversible manner, displaying much reduced potency against human chymotrypsin, cathepsin G, leukocyte elastase, and thrombin (Ki = 0.32, 0.63, 2.3, and 13 µM, respectively, vs. 620 nM using rabbit muscle 20S). A widely used inhibitor both in cultures in vitro and in animals in vivo.
Catalogue Number504314
Brand Family Calbiochem®
SynonymsBTZ, LDP-341, LDP341, MG341, MLN-341, MLN341, PS341, Proteasome Inhibitor XXII, PS-341, MG-341, Pyz-Phe-boroLeu, (R)-3-Methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butylboronic acid
References
ReferencesDu, X.L, and Chen, Q. 2013. Acta Haematol. 129, 207.
Tamatani, T., et al. 2013. Int. J. Oncol. 42, 935.
Beck, P., et al. 2012. J. Biol. Chem. 393, 1101.
Fang, H.T., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 2521.
Chen, D., et al. 2011. Curr. Cancer Drug Targets 11, 239.
Demo, S.D., et al. 2007. Cancer Res. 67, 6383.
Adams, J., et al. 1999. Cancer Res. 59, 2615.
Teicher, B.A., et al. 1999. Clin. Cancer Res. 5, 2638.
Adams, J., et al. 1998. Bioorg. Med. Chem. Lett. 8, 333.
Product Information
CAS number179324-69-7
FormOff-white solid
Hill FormulaC₁₉H₂₅BN₄O₄
Chemical formulaC₁₉H₂₅BN₄O₄
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationBortezomib, CAS 179324-69-7, is a cell-permeable, selective, slowly reversible inhibitor of 20S proteasome β5 ChTL/chymotrypsin- over β1 CL/caspase- and β2 TL/trypsin-like activity.
Biological Information
Primary Target20S proteasome
Purity≥98% by LC-MS
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Référence GTIN
5043140001 04055977263923

Documentation

Bortezomib - CAS 179324-69-7 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Bortezomib - CAS 179324-69-7 - Calbiochem Certificats d'analyse

TitreNuméro de lot
504314

Références bibliographiques

Aperçu de la référence bibliographique
Du, X.L, and Chen, Q. 2013. Acta Haematol. 129, 207.
Tamatani, T., et al. 2013. Int. J. Oncol. 42, 935.
Beck, P., et al. 2012. J. Biol. Chem. 393, 1101.
Fang, H.T., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 2521.
Chen, D., et al. 2011. Curr. Cancer Drug Targets 11, 239.
Demo, S.D., et al. 2007. Cancer Res. 67, 6383.
Adams, J., et al. 1999. Cancer Res. 59, 2615.
Teicher, B.A., et al. 1999. Clin. Cancer Res. 5, 2638.
Adams, J., et al. 1998. Bioorg. Med. Chem. Lett. 8, 333.
Fiche technique

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision29-March-2024 JSW
SynonymsBTZ, LDP-341, LDP341, MG341, MLN-341, MLN341, PS341, Proteasome Inhibitor XXII, PS-341, MG-341, Pyz-Phe-boroLeu, (R)-3-Methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butylboronic acid
DescriptionA cell-permeable dipeptidylboronate compound that selectively inhibits 20S proteasome β5 ChTL/chymotrypsin- over β1 CL/caspase- and β2 TL/trypsin-like activity (kinact/Ki = 38,000, 5,700, and <100 M-1s-1, respectively, in human 20S proteasome assays using 10 µM Suc-LLVY-AMC/Cat. No. 539142, 10 µM Z-LLE-AMC/Cat. No. 539141, or 50 µM Boc-LRR-AMC as substrate; IC50 in 1 h = 7, 74, and 4,200 nM, respectively) via a covalent, slowly reversible, interaction between the nucleophilic Thr1 hydroxy group/Thr1Oγ of the catalytic β subunit and the inhibitor's electrophilic boronic moiety, displaying much reduced potency against human chymotrypsin, cathepsin G, leukocyte elastase, and thrombin (Ki = 0.32, 0.63, 2.3, and 13 µM, respectively, vs. 620 nM using rabbit muscle 20S). A widely used inhibitor both in cultures in vitro and in animals in vivo. Despite being the first proteasome inhibitor approved by FDA for clinical anticancer treatment, its therapeutic efficacy continues to be hampered by off-target effects and dose-limiting toxicity.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number179324-69-7
Chemical formulaC₁₉H₂₅BN₄O₄
Structure formulaStructure formula
Purity≥98% by LC-MS
SolubilityDMSO (100 mg/ml) or Ethanol (2 mg/ml; with sonication). Use only fresh DMSO or Ethanol for reconstitution.
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesDu, X.L, and Chen, Q. 2013. Acta Haematol. 129, 207.
Tamatani, T., et al. 2013. Int. J. Oncol. 42, 935.
Beck, P., et al. 2012. J. Biol. Chem. 393, 1101.
Fang, H.T., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 2521.
Chen, D., et al. 2011. Curr. Cancer Drug Targets 11, 239.
Demo, S.D., et al. 2007. Cancer Res. 67, 6383.
Adams, J., et al. 1999. Cancer Res. 59, 2615.
Teicher, B.A., et al. 1999. Clin. Cancer Res. 5, 2638.
Adams, J., et al. 1998. Bioorg. Med. Chem. Lett. 8, 333.