product name
硼替佐米,
检测方案
≥98% (LC/MS)
质量水平
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
off-white
溶解性
DMSO: 100 mg/mL
ethanol: 2 mg/mL (with sonication)
储存温度
−20°C
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
一般描述
Bortezomib, a cell-permeable dipeptidylboronate compound, is a proteasome inhibitor. The proteasomal system is crucial for cellular protein turnover, which is necessary for maintaining cell homeostasis. Bortezomib binds reversibly to the chymotrypsin-like subunit of the 26S proteasome, inhibiting its function and thereby preventing the degradation of multiple pro-apoptotic factors. Bortezomib 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 M Suc-LLVY-AMC/Cat. No. 539142, 10 M Z-LLE-AMC/Cat. No. 539141, or 50 M 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 M, 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.
应用
Bortezomib has been used to induce aerobic glycolysis/ neuropathic pain in mice and study chemotherapy-induced painful peripheral neuropathy.
生化/生理作用
可逆性：是
细胞可渗透性：具有
特点和优势
- Cell permeable and enables targeted action
- Allows reversible modulation of cellular processes
包装
用惰性气体包装
警告
毒性：标准处理（A）
制备说明
仅使用新鲜的DMSO或乙醇用于重悬。
重悬
在重悬后分装并冻存于冰箱（-20°C.）储备溶液在-20°C下可稳定保存至多6个月。
其他说明
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 Targets11, 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.Cancer Res.5, 2638.
Adams, J., et al. 1998.Bioorg.Med. Chem. Lett.8, 333.
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 Targets11, 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.Cancer Res.5, 2638.
Adams, J., et al. 1998.Bioorg.Med. Chem. Lett.8, 333.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Susan D Demo et al.
Cancer research, 67(13), 6383-6391 (2007-07-10)
Clinical studies with bortezomib have validated the proteasome as a therapeutic target for the treatment of multiple myeloma and non-Hodgkin's lymphoma. However, significant toxicities have restricted the intensity of bortezomib dosing. Here we describe the antitumor activity of PR-171, a
Panjamurthy Kuppusamy et al.
Frontiers in pain research (Lausanne, Switzerland), 5, 1424348-1424348 (2024-07-09)
Chemotherapy-induced peripheral neuropathy (CIPN) is a debilitating side effect of cancer treatment that significantly impacts patients' quality of life. This study investigated the effects of targeting metabolic pathways on bortezomib-induced neuropathic pain and tumor growth using a Lewis lung carcinoma
J Adams et al.
Bioorganic & medicinal chemistry letters, 8(4), 333-338 (1999-01-01)
Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.
Philipp Beck et al.
Biological chemistry, 393(10), 1101-1120 (2012-10-24)
The 20S proteasome core particle (CP) is the proteolytically active key element of the ubiquitin proteasome system that directs the majority of intracellular protein degradation in eukaryotic cells. Over the past decade, the CP has emerged as an anticancer therapy
D Chen et al.
Current cancer drug targets, 11(3), 239-253 (2011-01-21)
Targeting the ubiquitin-proteasome pathway has emerged as a rational approach in the treatment of human cancer. Based on positive preclinical and clinical studies, bortezomib was subsequently approved for the clinical use as a front-line treatment for newly diagnosed multiple myeloma
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