硼替佐米|T2399

Bortezomib
179324-69-7

￥413 5mg 起订

￥546 10mg 起订

￥962 25mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 硼替佐米

英文名称：: Bortezomib

CAS号：: 179324-69-7

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.97%

产品类别：: 抑制剂

货号：: T2399

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.
溶解度	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.1 mg/mL (18.48 mM), Working solution is recommended to be prepared and used immediately. H2O : Insoluble Ethanol : 20.83 mg/ml (54.21 mM), Sonication is recommended. DMSO : 71 mg/mL (184.8 mM)
关键字	Nuclear factor-kappaB \| Inhibitor \| LDP-341 \| Nuclear factor-κB \| Apoptosis \| LDP341 \| PS 341 \| PS341 \| Bortezomib \| Autophagy \| Proteasome \| MG341 \| PS-341 \| inhibit \| NF-κB \| NSC-681239 \| NSC681239 \| MG-341
相关产品	Guanidine hydrochloride \| Hydroxychloroquine
相关库	抑制剂库 \| 抗癌上市药物库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 抗癌临床化合物库 \| 抗癌药物库

Radiciol|||NSC 681239|||MG 341|||DPBA|||硼替佐米|||Brotezamide|||LDP 341|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
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