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Bortezomib

Bortezomib

产品编号 T2399   CAS 179324-69-7
别名: Radiciol, NSC 681239, 硼替佐米, MG 341, DPBA, Brotezamide, LDP 341

Bortezomib (LDP 341) 是一种 20S 蛋白酶体抑制剂 (Ki=0.6 nM),具有可逆性和选择性。Bortezomib 具有抗肿瘤活性,可以抑制 NF-κB,可破坏细胞周期、诱导细胞凋亡

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Bortezomib Chemical Structure
Bortezomib, CAS 179324-69-7
规格 价格/CNY 货期 数量
1 mg ¥ 188 现货
5 mg ¥ 413 现货
10 mg ¥ 546 现货
25 mg ¥ 962 现货
50 mg ¥ 1,490 现货
100 mg ¥ 2,380 现货
200 mg ¥ 3,650 现货
500 mg ¥ 5,830 现货
1 mL * 10 mM (in DMSO) ¥ 413 现货
其他形式的 Bortezomib:
产品目录号及名称: Bortezomib (T2399)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.
靶点活性 20S proteasome:0.6 nM (cell free)
体外活性 方法:人舌鳞癌细胞 SCC-15 和 CAL-27、人咽鳞癌细胞 FaDu、人唾液腺癌细胞 A-253 和 SALTO-5 用 Bortezomib (6.25-100 nM) 处理 24-72 h,使用 SRB 方法检测细胞生长抑制情况。
结果:Bortezomib 对五种肿瘤细胞增殖的影响是剂量和时间依赖性的。SCC-15 是对 Bortezomib 作用最敏感的细胞。[1]
方法:人小细胞肺癌细胞 NCI-H69 和 NCI-H2171 用 Bortezomib (0.05 μM; 0.5 μM) 处理 48 h,使用 Flow Cytometry 方法检测细胞周期和细胞凋亡情况。
结果:Bortezomib 引起 G2-M 过渡状态下的细胞周期停滞,G2 期细胞增加,S 期细胞减少。Bortezomib 诱导肿瘤细胞凋亡。[2]
方法:人大细胞肺癌细胞 H460 用 Bortezomib (0.01-10 μM) 孵育 3-48 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Bortezomib 处理导致 Bcl-2 蛋白的浓度依赖性磷酸化。从 12 h 开始,观察到可辨别的 Bcl-2 切割产物,Bcl-2 磷酸化先于 Bcl-2 切割至少 9 h。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 Bortezomib (0.3 mg/kg) 腹腔注射给携带原发性渗出性淋巴瘤 (PEL) UM-PEL-1 的 NOD/SCID 小鼠,每天一次,持续三周。
结果:Bortezomib 诱导 PEL 缓解,并延长淋巴瘤渗出小鼠的总生存期。Bortezomib 下调细胞周期进程、DNA 复制和 Myc 靶基因。[4]
方法:为研究 Bortezomib 对肾纤维化的影响,将 Bortezomib (0.5 mg/kg) 腹腔注射给马兜铃酸I (AA)诱导的纤维化 C57BL/6J 小鼠模型,每周两次,持续十周。
结果:Bortezomib 治疗显著减轻了 AA 诱导的肾功能障碍和蛋白尿,降低了肾纤维化相关蛋白和肾损伤标志物的表达,如 αSMA、Kim1 和 Ngal,并在组织病理学水平上预防了肾纤维化。[5]
激酶实验 Inhibitors were synthesized and purified according to the procedures described in Adams et al.The inhibition constant (Ki) for each inhibitor was measured according to the method of Stein et al.using a fluorometric assay,monitoring peptide substrate cleavage of Z-Leu-Leu-Val-Tyr-amino methyl coumarin (Z = carbobenzyloxy) by the 20S proteasome [1].
细胞实验 PC-3 cells were treated with different doses of PS-341 for different periods of time. The cells were washed with PBS, harvested, and fixed in suspension with 3.7% formaldehyde in the neutral buffer for 10 min at room temperature. The cells were centrifuged, and the cell pellet was resuspended in 0.5 ml of 80% ethanol. The cell suspension (25–50 μl) was then placed onto a microscope slide precoated with poly-l-lysine and air-dried. The slides were washed four times with 0.1% Triton X-100 in PBS. The slide was incubated with the DNA stain Hoechst 33342 (Molecular Probes; 1.0 μg/ml in PBS with 0.1% Triton-X-100) for 1.0 min. The slides were rinsed in PBS and mounted with 70% glycerol containing 25 mg/ml 1,4-diazabicyclo[2.2.2]octane. Nuclear staining was visualized using a fluorescent microscope [1].
动物实验 Mice were inoculated s.c. into the right flank with 3 × 10^7 MM cells in 100 μl of RPMI 1640, together with 100 μl of Matrigel basement membrane matrix. When tumor was measurable, mice were assigned into four treatment groups receiving PS-341 or into a control group. Treatment with PS-341 was given i.v. twice weekly via tail vein at 0.05, 0.1, 0.5, and 1.0 mg/kg for 4 weeks. Subsequently, it was administered once weekly. The control group received the vehicle alone (0.9% sodium chloride) at the same schedule. Caliper measurements of the longest perpendicular tumor diameters were performed every alternate day to estimate the tumor volume, using the following formula: 4π/3 × (width/2)^2 × (length/2), representing the three-dimensional volume of an ellipse. Animals were sacrificed when their tumors reached 2 cm or when the mice became moribund. Survival was evaluated from the first day of treatment until death [4].
别名 Radiciol, NSC 681239, 硼替佐米, MG 341, DPBA, Brotezamide, LDP 341
化合物与蛋白结合的复合物

T2399_1

Crystal structure of CTX-M-14 in complex with Bortezomib

分子量 384.24
分子式 C19H25BN4O4
CAS No. 179324-69-7

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

Ethanol: Insoluble

DMSO: 71 mg/mL (184.8 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6025 mL 13.0127 mL 26.0254 mL 65.0635 mL
5 mM 0.5205 mL 2.6025 mL 5.2051 mL 13.0127 mL
10 mM 0.2603 mL 1.3013 mL 2.6025 mL 6.5064 mL
20 mM 0.1301 mL 0.6506 mL 1.3013 mL 3.2532 mL
50 mM 0.0521 mL 0.2603 mL 0.5205 mL 1.3013 mL
100 mM 0.026 mL 0.1301 mL 0.2603 mL 0.6506 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Benvenuto M, et al. Proteasome inhibition by bortezomib parallels a reduction in head and neck cancer cells growth, and an increase in tumor-infiltrating immune cells. Sci Rep. 2021 Sep 24;11(1):19051. 2. Taromi S, et al. Proteasome inhibitor bortezomib enhances the effect of standard chemotherapy in small cell lung cancer. Oncotarget. 2017 Sep 23;8(57):97061-97078. 3. Ling YH, et al. PS-341, a novel proteasome inhibitor, induces Bcl-2 phosphorylation and cleavage in association with G2-M phase arrest and apoptosis. Mol Cancer Ther. 2002 Aug;1(10):841-9. 4. Sarosiek KA, et al. Efficacy of bortezomib in a direct xenograft model of primary effusion lymphoma. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13069-74. 5. Zeniya M, et al. The proteasome inhibitor bortezomib attenuates renal fibrosis in mice via the suppression of TGF-β1. Sci Rep. 2017 Oct 12;7(1):13086. 6. Qu, Yuan Qing, et al. 2-Aminoethoxydiphenylborane sensitizes anti-tumor effect of bortezomib via suppression of calcium-mediated autophagy. Cell death & disease. 2018 Mar 2;9(3):361.

文献引用

1. Zhou Q, Liang J, Yang T, et al. Carfilzomib modulates tumor microenvironment to potentiate immune checkpoint therapy for cancer. EMBO Molecular Medicine. 2022 Jan 11;14(1):e14502. doi: 10.15252/emmm.202114502. Epub 2021 Dec 13. 2. Li Q, Chu Y, Li S, et al. The oncoprotein MUC1 facilitates breast cancer progression by promoting Pink1-dependent mitophagy via ATAD3A destabilization. Cell Death & Disease. 2022, 13(10): 1-16. 3. Qu, Yuan Qing, et al. 2-Aminoethoxydiphenylborane sensitizes anti-tumor effect of bortezomib via suppression of calcium-mediated autophagy. Cell Death & Disease. 2018, 9(3): 1-15 4. Zhang L, Xu L, Zhang X, et al. Methyltransferase Setdb1 Promotes Osteoblast Proliferation by Epigenetically Silencing Macrod2 with the Assistance of Atf7ip. Cells. 2022, 11(16): 2580. 5. Chen X, Chen Y, Ou Y, et al. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochemical Pharmacology. 2022, 206: 115326. 6. Liu M, Zhao Y T, Lv Y Y, et al. Metformin Relieves Bortezomib-Induced Neuropathic Pain by Regulating AMPKa2-Mediated Autophagy in the Spinal Dorsal Horn. Neurochemical Research. 2022: 1-10. 7. Sassetti E, Durante Cruz C, Identification and Characterization of Approved Drugs and Drug-Like Compounds as Covalent Escherichia coli ClpP Inhibitors. International Journal of Molecular Sciences. 2019, 20(11): 2686 8. Wang M, Wang J, Tsui A Y P, et al. Mechanisms of peripheral neurotoxicity associated with four chemotherapy drugs using human induced pluripotent stem cell-derived peripheral neurons. Toxicology in Vitro. 2021: 105233. 9. Liang Y, Qian Y, Tang J, et al.Arsenic trioxide promotes ERK1/2-mediated phosphorylation and degradation of BIMEL to attenuate apoptosis in BEAS-2B cells.Chemico-Biological Interactions.2022: 110304. 10. He Y, Shi Q, Ling Y, et al.ABLIM1, a novel ubiquitin E3 ligase, promotes growth and metastasis of colorectal cancer through targeting IĸBα ubiquitination and activating NF-ĸB signaling.Cell Death & Differentiation.2024: 1-14.
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ASK1-IN-2 BQZ-485 LCH-7749944 TPCA-1 Salinomycin sodium salt Pomalidomide Parthenolide 3-Bromopyruvic acid

相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 抗癌临床化合物库 抗癌药物库 抗癌活性化合物库 上市药物库 抗抑郁症化合物库 抗衰老化合物库 FDA上市及药典收录分子库 抗乳腺癌化合物库 药物功能重定位化合物库

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Bortezomib 179324-69-7 Apoptosis Autophagy NF-Κb Proteases/Proteasome Ubiquitination NF-κB Proteasome Nuclear factor-kappaB Inhibitor LDP-341 Nuclear factor-κB LDP341 PS 341 PS341 Radiciol MG341 PS-341 NSC 681239 硼替佐米 inhibit MG 341 DPBA NSC-681239 NSC681239 Brotezamide LDP 341 MG-341 inhibitor

 

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