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504314 Bortezomib - CAS 179324-69-7 - Calbiochem

504314
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Empirical FormulaCAS #
C₁₉H₂₅BN₄O₄ 179324-69-7

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      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≥99% by HPLC
      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

      Documentation

      Bortezomib - CAS 179324-69-7 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Bortezomib - CAS 179324-69-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      504314

      References

      Reference overview
      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.
      Data Sheet

      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.

      Revision04-July-2013 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≥99% by HPLC
      SolubilityDMSO (100 mg/ml) or Ethanol (2 mg/ml; with sonication). Use only fresh DMSO or Ethanol for reconstitution.
      Storage -20°C
      Hygroscopic
      Protect from light
      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.