硼替佐米 T2399
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
1 mL | 179324-69-7 | ¥413.00 | 询底价 |
100 mg | 179324-69-7 | ¥2,380.00 | 询底价 |
200 mg | 179324-69-7 | ¥3,650.00 | 询底价 |
25 mg | 179324-69-7 | ¥962.00 | 询底价 |
1 mg | 179324-69-7 | ¥188.00 | 询底价 |
5 mg | 179324-69-7 | ¥413.00 | 询底价 |
10 mg | 179324-69-7 | ¥546.00 | 询底价 |
500 mg | 179324-69-7 | ¥5,830.00 | 询底价 |
50 mg | 179324-69-7 | ¥1,490.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Bortezomib
描述: 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。
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 sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: 5% DMSO+95% Saline : 3.55 mg/mL (9.24 mM, suspension)
H2O : Insoluble
Ethanol : Insoluble
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: COTI-2 | Polyphyllin I | Tubulin inhibitor 32 | Glyphosate | BMS-833923 | Rosmarinic acid | EGFR-IN-3 | Sandalore | Pivanex | DPN
相关库: Drug Repurposing Compound Library | Anti-Prostate Cancer Compound Library | Targeted Therapy Drug Library | Anti-Cancer Drug Library | Cardiotoxicity Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途