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/ Bortezomib

硼替佐米 /Bortezomib 98%

货号：A385479 同义名： PS-341;LDP-341 Ambeed 开学季，买赠积分，赢豪礼

Bortezomib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 主要用于多发性骨髓瘤和其他血液癌症的治疗研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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Excepted Quantity USD 0.00
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Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Bortezomib 化学结构 CAS号：179324-69-7
Bortezomib 化学结构
CAS号：179324-69-7
Bortezomib 3D分子结构
CAS号：179324-69-7
Bortezomib 化学结构 CAS号：179324-69-7
Bortezomib 3D分子结构 CAS号：179324-69-7
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Bortezomib 纯度/质量文件 产品仅供科研

货号：A385479 标准纯度： 98%
批次查询： 批次纯度:

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产品名称 20S proteasome ↓ Proteasome ↓ 其他靶点 纯度
Ixazomib ++++

20S proteasome, Ki: 0.93 nM

20S proteasome, IC50: 3.4 nM

 		99%+
Delanzomib +++

Chymotrypsin-like proteasome, IC50: 3.8 nM

 		98%
Celastrol +

20S proteasome, IC50: 2.5 μM

 		98%
MLN9708 +++

20S proteasome, Ki: 0.93 nM

20S proteasome, IC50: 3.4 nM

 		99%
Bortezomib ++++

20S proteasome, Ki: 0.6 nM

 		98%
Oprozomib ++

20S proteasome LMP7, IC50: 82 nM

20S proteasome β5, IC50: 36 nM

 		99%+
Epoxomicin ✔ 99%
PI-1840 ++

Chymotrypsin-like proteasome, IC50: 27 nM

 		98%
VR23 +++

Chymotrypsin-like proteasomes, IC50: 3 μM

Trypsin-like proteasomes, IC50: 1 nM

 		98%
Carfilzomib ++

Proteasome, IC50: 5 nM

 		98%
(R)-MG-132 +

Proteasome, IC50: 100 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Bortezomib 生物活性

靶点

  • 20S proteasome

    20S proteasome, Ki:0.6 nM
描述 The proteasome is a catalytic enzyme complex responsible for the degradation of intracellular proteins. Bortezomib is a dipeptide boronate that potently inhibits proteasome with a Ki value of 0.6 nM. After 48-hour incubation, bortezomib at 0.1 μM completed inhibited the growth of different human multiple myeloma (MM) cell lines, including U266, IM-9 and Hs Sultan cells. In U266 and patient primary MM cells, the treatment of 0.01 μM bortezomib induced a progressive increase of sub-G0/G1 phase cells in a time-dependent manner from 0 – 16h. Apoptosis as indicated by DNA fragmentation was also promoted by bortezomib treatment. H460 cells treated by 0.01 – 10 μM bortezomib for 24 hours showed increased cell accumulation at G2-M phase and cell apoptosis in a dose-dependent manner compared to control cells. Bortezomib treatment also led to concentration-dependent phosphorylation of Bcl-2 proteins. When cells were exposed to higher doses of bortezomib (0.1 – 10 μM) for 24 hours, the superphosphorylated form of Bcl-2 was detected. After the exposure to 0.01 – 0.05 μM bortezomib for 24 hours, or 0.1 μM bortezomib for 12 hours, the first cleavage fragment of Bcl-2 protein was detected. The second cleave fragment of Bcl-2 was only found in cells treated with 0.1 μM bortezomib for 12 hours. After incubating with 0.1 μM bortezomib for 24 hours, the phosphorylated Bcl-2 bands were observed in both Triton-X-100 soluble and insoluble fraction. In vivo study showed that 3 times per week injection of 2 mg/kg bortezomib for 25 days inhibited the growth of murine and human squamous cell carcinoma in mice.
作用机制 Bortezomib inhibits proteasome by reversibly binding to the chymotrypsin-like subunit of the proteasome.

Bortezomib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 Growth Inhibition Assay IC50=1.99 nM SANGER
8-MG-BA Growth Inhibition Assay IC50=0.25 nM SANGER
A101D Growth Inhibition Assay IC50=0.225 nM SANGER
A253 Growth Inhibition Assay IC50=0.208 nM SANGER

Bortezomib 动物研究

Dose Mice: 0.25 mg/kg - 1 mg/kg[6] (i.v.), 1 mg/kg[7] (i.p.) Rat: 0.1 mg/kg, 0.2 mg/kg[8] (i.p.)
Administration i.v., i.p.

Bortezomib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00571493 Non-hodgkin's Lymphoma ... 展开 >> Mantle Cell Lymphoma 收起 << Phase 1 Phase 2 Completed - United States, Nebraska ... 展开 >> University of Nebraska Medical Center, Section of Oncology/Hematology Omaha, Nebraska, United States, 68198-7680 收起 <<
NCT00580320 Melanoma Soft... 展开 >> Tissue Sarcoma Parathyroid Carcinoma Small Cell Carcinoma of the Lung Carcinoid Tumors 收起 << Phase 1 Completed - United States, New Hampshire ... 展开 >> Dartmouth Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756 United States, Virginia Massey Cancer Center/Virginia Commonwealth University Richmond, Virginia, United States, 23298 收起 <<
NCT02808091 Extranodal NK-T-CELL LYMPHOMA Phase 2 Terminated(Slow recruitment) - Singapore ... 展开 >> National Cancer Centre Singapore, Singapore, 169610 收起 <<

Bortezomib 参考文献

[1]Ludwig H, Khayat D, et al. Proteasome inhibition and its clinical prospects in the treatment of hematologic and solid malignancies. Cancer. 2005;104(9):1794-807.

[2]Hideshima T, Richardson P, et al. The proteasome inhibitor PS-341 inhibits growth, induces apoptosis, and overcomes drug resistance in human multiple myeloma cells. Cancer Res. 2001;61(7):3071-6.

[3]Ling YH, Liebes L, et al. PS-341, a novel proteasome inhibitor, induces Bcl-2 phosphorylation and cleavage in association with G2-M phase arrest and apoptosis. Mol Cancer Ther. 2002;1(10):841-9.

[4]Sunwoo JB, Chen Z, et al. Novel proteasome inhibitor PS-341 inhibits activation of nuclear factor-kappa B, cell survival, tumor growth, and angiogenesis in squamous cell carcinoma. Clin Cancer Res. 2001;7(5):1419-28.

[5]Accardi F, Toscani D, et al. Mechanism of Action of Bortezomib and the New Proteasome Inhibitors on Myeloma Cells and the Bone Microenvironment: Impact on Myeloma-Induced Alterations of Bone Remodeling. Biomed Res Int. 2015.

Bortezomib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.03mL

5.21mL

2.60mL

Bortezomib 技术信息

CAS号179324-69-7
分子式C19H25BN4O4
分子量 384.237
别名 PS-341;LDP-341;MLN 341. US brand name: VELCADE.;MLN341;MG-341;NSC 681239
运输蓝冰
存储条件

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 50 mg/mL(130.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 60 mg/mL(156.15 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 11 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

Tags: Bortezomib | PS-341;LDP-341;MLN 341. MLN341;MG-341;NSC 681239 | Apoptosis Inducer | Proteasome | AmBeed-信号通路专用抑制剂 | Bortezomib 纯度/质量文件 | Bortezomib 亚型比较 | Bortezomib 生物活性 | Bortezomib 细胞研究 | Bortezomib 动物研究 | Bortezomib 临床数据 | Bortezomib 参考文献 | Bortezomib 实验方案 | Bortezomib 技术信息

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