1. Metabolic Enzyme/Protease NF-κB Apoptosis Autophagy
  2. Proteasome NF-κB Apoptosis Autophagy
  3. Bortezomib

Bortezomib  (Synonyms: 硼替佐米; PS-341; LDP-341; NSC 681239)

目录号: HY-10227 纯度: 99.83%
COA 产品使用指南

Bortezomib (PS-341) 是一种可逆性和选择性的蛋白酶体 (proteasome) 抑制剂,通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki=0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一种蛋白酶体抑制剂,具有抗癌活性。

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Bortezomib Chemical Structure

Bortezomib Chemical Structure

CAS No. : 179324-69-7

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 118 篇科研文献

WB
IF
Proliferation Assay

    Bortezomib purchased from MCE. Usage Cited in: Mol Cell Biochem. 2023 May 19.  [Abstract]

    Bortezomib (BTZ; 10 nM; 48 h) significantly enhances the cell death of RPMI-8226.

    Bortezomib purchased from MCE. Usage Cited in: Mol Cell Biochem. 2023 May 19.  [Abstract]

    Bortezomib (BTZ; 5, 10, 20 nM; 48 h) increases the expression level of γH2AX in RPMI-8226 and U266 cells.

    Bortezomib purchased from MCE. Usage Cited in: Clin Cancer Res. 2019 Jun 15;25(12):3630-3642.  [Abstract]

    H1975 cells treated with 5 μmol/L MTI-31 alone or in combination with 10 μmol/L CQ or 0.01 μmol/L PS-341.

    Bortezomib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.  [Abstract]

    Different concentrations of two classical proteasome inhibitors Bortezomib and MG132 are added. AGS cells are either untreated or treated with Bortezomib (25 nM) or MG132 (0.1 μM) for 24 h in the absence or presence of baf A1 (100 nM).

    Bortezomib purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.  [Abstract]

    AGS cells are pretreated with 25 and 50 nM Bortezomib for 1 h, and then incubated with 500 nM Torin 1 for 24 h. After pretreatment with PPI for 24 h in pH 7.4 or pH 6.5 condition, Rapamycin (1 μM) or Torin 1 (500 nM) is added for another 24 h. The protein level of SQSTM1 is measured by western blot analysis.

    Bortezomib purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    Kelly cells are treated with increasing concentrations of Thalidomide and co-treated with 5 μM Bortezomib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Bortezomib purchased from MCE. Usage Cited in: BMC Cancer. 2018 Oct 11;18(1):971.  [Abstract]

    The reduction of MAGEC2 protein level in TRIM28-knockdown A375 cells can be inhibited by treatment with both MG132 and PS-341, and similar result is also observed in Hs 695 T cells.

    Bortezomib purchased from MCE. Usage Cited in: Eur J Pharmacol. 2017 Nov 15;815:147-155.  [Abstract]

    Shown are GFPu fluorescent images of the GFPu-HEK293 cells treated with CuSO4 (Cu, 20 μM), HK (20 μM), HK-Cu (HC, 20 μM), or Velcade (Vel, 100 nM).

    查看 NF-κB 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].

    IC50 & Target

    Ki: 0.6 nM (20S proteasome)[1]

    体外研究
    (In Vitro)

    Bortezomib (PS-341) (100 nM;8 小时) 导致 G2-M 期细胞积累,G1 期细胞数量相应减少[1]
    Bortezomib (PS-341) (5-100 nM;20 小时) 在套细胞淋巴瘤 (MCL) 细胞系中诱导细胞凋亡[3]
    Bortezomib (PS-341) (20 nM;1-14 小时) 在两种 MCL 细胞系[3]中诱导 Noxa 上调。
    Bortezomib (PS-341) 的 IC50 是发现 B16F10 细胞中 26S 蛋白酶体的浓度为 2.46 nM[4]
    Bortezomib (PS-341) 抑制多种抗凋亡蛋白 (例如,Bcl-XL、Bcl-2、和 STAT-3)[5]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Cycle Analysis[1]

    Cell Line: PC-3 cells
    Concentration: 100 nM
    Incubation Time: 8 hours
    Result: Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.

    Apoptosis Analysis[3]

    Cell Line: JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines)
    Concentration: 5-100 nM
    Incubation Time: 20 hours
    Result: The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM).

    Western Blot Analysis[3]

    Cell Line: wtp53 (Granta-519), mutp53 (Jeko) cells
    Concentration: 20 nM
    Incubation Time: 1, 2, 4, 6, 14 hours
    Result: Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).
    体内研究
    (In Vivo)

    Bortezomib (PS-341) (0.3-1 mg/kg;静脉注射;每周一次,持续 4 周) 抑制裸鼠体内的 PC-3 肿瘤生长[1]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male nude mice (xenograft tumor model bearing PC-3 cells)[1]
    Dosage: 0.3, 1 mg/kg
    Administration: Intravenous injection; once weekly for 4 weeks
    Result: Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg.
    Clinical Trial
    分子量

    384.24

    Formula

    C19H25BN4O4

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    硼替佐米;保特佐米

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    In Vitro: 

    Ethanol 中的溶解度 : 66.67 mg/mL (173.51 mM; 超声助溶 (<60°C))

    DMSO 中的溶解度 : 50 mg/mL (130.13 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6025 mL 13.0127 mL 26.0254 mL
    5 mM 0.5205 mL 2.6025 mL 5.2051 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 4 mg/mL (10.41 mM); 澄清溶液

      此方案可获得 ≥ 4 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 40.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 4 mg/mL (10.41 mM); 澄清溶液

      此方案可获得 ≥ 4 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 40.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.97%

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 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
    15 mM 0.1735 mL 0.8675 mL 1.7350 mL 4.3376 mL
    20 mM 0.1301 mL 0.6506 mL 1.3013 mL 3.2532 mL
    25 mM 0.1041 mL 0.5205 mL 1.0410 mL 2.6025 mL
    30 mM 0.0868 mL 0.4338 mL 0.8675 mL 2.1688 mL
    40 mM 0.0651 mL 0.3253 mL 0.6506 mL 1.6266 mL
    50 mM 0.0521 mL 0.2603 mL 0.5205 mL 1.3013 mL
    60 mM 0.0434 mL 0.2169 mL 0.4338 mL 1.0844 mL
    80 mM 0.0325 mL 0.1627 mL 0.3253 mL 0.8133 mL
    100 mM 0.0260 mL 0.1301 mL 0.2603 mL 0.6506 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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