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Bortezomib

产品编号 T2399Cas号 179324-69-7
别名 Radiciol, NSC 681239, MG 341, DPBA, 硼替佐米, 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。

Bortezomib

Bortezomib

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

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。

规格价格库存数量
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 x 10 mM (in DMSO)¥ 413现货
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产品介绍

生物活性
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, MG 341, DPBA, 硼替佐米, Brotezamide, LDP 341
化学信息
分子量384.24
分子式C19H25BN4O4
CAS No.179324-69-7
储存&溶解度
存储keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
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)
溶液配制表
10% DMSO+40% PEG300+5% Tween 80+45% Saline/Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.6025 mL13.0127 mL26.0254 mL130.1270 mL
5 mM0.5205 mL2.6025 mL5.2051 mL26.0254 mL
10 mM0.2603 mL1.3013 mL2.6025 mL13.0127 mL
Ethanol/DMSO
1mg5mg10mg50mg
20 mM0.1301 mL0.6506 mL1.3013 mL6.5064 mL
50 mM0.0521 mL0.2603 mL0.5205 mL2.6025 mL
DMSO
1mg5mg10mg50mg
100 mM0.0260 mL0.1301 mL0.2603 mL1.3013 mL

计算器

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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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

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% DMSO
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