504314 | Bortezomib - CAS 179324-69-7 - Calbiochem

504314
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₂₅BN₄O₄ 179324-69-7

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04314.0001
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          Glass bottle 5 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.