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- CAS号：
179324-69-7
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mg | 产品价格： | ￥169.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥330.0 |
| 规格： | 5mg | 产品价格： | ￥330.0 |
| 规格： | 10mg | 产品价格： | ￥436.0 |
| 规格： | 25mg | 产品价格： | ￥769.0 |
| 规格： | 50mg | 产品价格： | ￥1192.0 |
| 规格： | 100mg | 产品价格： | ￥1904.0 |
| 规格： | 200mg | 产品价格： | ￥2920.0 |
| 规格： | 500mg | 产品价格： | ￥4664.0 |
Product Introduction
Bioactivity
| 名称 | Bortezomib |
| 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. |
| 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]. |
| 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]. |
| 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]. |
| 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] |
| 存储条件 | Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.1 mg/mL (18.48 mM), Solution. H2O : Insoluble Ethanol : 20.83 mg/mL (54.21 mM), Sonication is recommended. DMSO : 255 mg/mL (663.65 mM), Sonication is recommended. |
| 关键字 | PS-341 | PS341 | PS 341 | Proteasome | Nuclear factor-κB | Nuclear factor-kappaB | NSC-681239 | NSC681239 | NF-κB | NFκB | NF-kB | NFkB | MG-341 | MG341 | LDP-341 | LDP341 | Inhibitor | inhibit | Bortezomib | Autophagy | Apoptosis | 20S proteasome |
| 相关产品 | Formamide | D-Psicose | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Metronidazole | Hemin | Hydroxychloroquine | Stavudine | Paeonol | Ethyl linoleate |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Failed Clinical Trials Compound Library | EMA Approved Drug Library | Anti-Aging Compound Library | Anti-Viral Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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相关实验
王红阳院士等 Science 子刊报道老药新用的精准治疗机制，为 PTEN 突变肿瘤治疗带来新思路
）, 并将其用于药物筛选和分子谱分析，以寻找个性化的治疗方法和治疗机制。通过使用69种经过FDA批准的抗癌药库，对96孔板中培养的10个PDCs进行药物筛选测定，作者发现蛋白酶体抑制剂硼替佐米（bortezomib，多发性骨髓瘤治疗药物）对PDCs具有强大的细胞毒性作用。通过对胆管癌细胞系验证发现，不同细胞系对蛋白酶抑制剂的敏感性有所不同。 图片来源：Science Translational Medicine为了探究导致敏感性差异的机制，作者对两种代表性细胞系HCCC-9810（敏感）和RBE（不敏感）的进
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￥169 - 4664
