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504314 Sigma-AldrichBortezomib - 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 MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet

同义词: 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

Recommended Products

概述

Replacement Information

重要规格表

CAS #	Empirical Formula
179324-69-7	C₁₉H₂₅BN₄O₄

Products

产品目录编号	包装	数量 / 包装
5.04314.0001	玻璃瓶	5 mg	添加到收藏夹添加到收藏夹添加到我的收藏夹

Description
Overview	A cell-permeable dipeptidylboronate compound that selectively inhibits 20S proteasome β5 ChTL/chymotrypsin- over β1 CL/caspase- and β2 TL/trypsin-like activity (k_inact/K_i = 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 (K_i = 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 Number	504314
Brand Family	Calbiochem®
Synonyms	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

References
References	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.

References

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.

Product Information
CAS number	179324-69-7
Form	Off-white solid
Hill Formula	C₁₉H₂₅BN₄O₄
Chemical formula	C₁₉H₂₅BN₄O₄
Hygroscopic	Hygroscopic
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications
Application	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.

Biological Information
Primary Target	20S proteasome
Purity	≥98% by LC-MS

Physicochemical Information
Cell permeable	Y

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 Instructions	Following 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
产品目录编号	GTIN
5.04314.0001	04055977263923

Documentation

Bortezomib - CAS 179324-69-7 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

Bortezomib - CAS 179324-69-7 - Calbiochem 分析证书

标题	批号
504314	输入批号

参考

参考信息概述
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.

参考信息概述

数据表

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.

Revision	29-March-2024 JSW
Synonyms	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
Description	A cell-permeable dipeptidylboronate compound that selectively inhibits 20S proteasome β5 ChTL/chymotrypsin- over β1 CL/caspase- and β2 TL/trypsin-like activity (k_inact/K_i = 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/Thr1O^γ 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 (K_i = 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.
Form	Off-white solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	179324-69-7
Chemical formula	C₁₉H₂₅BN₄O₄
Structure formula
Purity	≥98% by LC-MS
Solubility	DMSO (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 Instructions	Following reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	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.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Proteases Inhibitors > Proteasome and Ubiquitination Pathway Inhibitors

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