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/ Bortezomib/硼替佐米

Bortezomib/硼替佐米 {[allProObj[0].p_purity_real_show]}

货号：A385479 同义名： PS-341; LDP-341

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.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
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/硼替佐米 化学结构 CAS号：179324-69-7
Bortezomib/硼替佐米 化学结构
CAS号：179324-69-7
Bortezomib/硼替佐米 3D分子结构
CAS号：179324-69-7
Bortezomib/硼替佐米 化学结构 CAS号：179324-69-7
Bortezomib/硼替佐米 3D分子结构 CAS号：179324-69-7
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Bortezomib/硼替佐米 纯度/质量文件 产品仅供科研

货号：A385479 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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产品名称 20S proteasome ↓ Proteasome ↓ 其他靶点 纯度
Ixazomib ++++

20S proteasome, IC50: 3.4 nM

20S proteasome, Ki: 0.93 nM

 		99%+
Delanzomib +++

Chymotrypsin-like proteasome, IC50: 3.8 nM

 		98%
Celastrol +

20S proteasome, IC50: 2.5 μM

 		98%
MLN9708 +++

20S proteasome, IC50: 3.4 nM

20S proteasome, Ki: 0.93 nM

 		99%
Bortezomib ++++

20S proteasome, Ki: 0.6 nM

 		98%
Oprozomib ++

20S proteasome β5, IC50: 36 nM

20S proteasome LMP7, IC50: 82 nM

 		99%+
Epoxomicin ✔ 95%
PI-1840 ++

Chymotrypsin-like proteasome, IC50: 27 nM

 		98%
VR23 +++

Trypsin-like proteasomes, IC50: 1 nM

Chymotrypsin-like proteasomes, IC50: 3 μM

 		99%
Carfilzomib ++

Proteasome, IC50: 5 nM

 		98%
(R)-MG-132 +

Proteasome, IC50: 100 nM

 		98% (NMR）
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/硼替佐米 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/硼替佐米 细胞实验

Cell Line
Concentration Treated Time Description References
5TGM1.BR cells 20nM bortezomib Continuous culture Evaluate bortezomib resistance Neoplasia. 2022;24(1):1-11.
ANBL6.BR cells 10nM bortezomib Continuous culture Evaluate bortezomib resistance Neoplasia. 2022;24(1):1-11.
Kas6.BR cells 10nM bortezomib Continuous culture Evaluate bortezomib resistance Neoplasia. 2022;24(1):1-11.
RPMI-8226.BR cells 10nM bortezomib Continuous culture Evaluate bortezomib resistance Neoplasia. 2022;24(1):1-11.
MM.1 S cells 0.5 nM 6 months Induce Bortezomib resistance, IC50 value increased more than 10 times Nat Commun. 2023 Mar 9;14(1):1290.
LP-1 cells 10 nM 24 h Evaluate the effect of HDAC1 inhibitor Rom combined with Bortezomib, significantly increased apoptosis rate Nat Commun. 2023 Mar 9;14(1):1290.
GBC-SD cells 0.01 μM 48 h To evaluate the antiproliferative effect of ES-NP(BTZ;Ce6) +NIR on GBC-SD cells, the results showed an IC50 value significantly lower than that of BTZ alone. Adv Sci (Weinh). 2022 Mar;9(7):e2103895.
NOZ cells 0.0048 μM 48 h To evaluate the antiproliferative effect of ES-NP(BTZ;Ce6) +NIR on NOZ cells, the results showed an IC50 value of 4.8 × 10^-9 M, significantly lower than 11.4 × 10^-9 M for BTZ alone. Adv Sci (Weinh). 2022 Mar;9(7):e2103895.
L1210 cells 10 nM 24 h To evaluate the cytotoxic effects of Bortezomib on L1210 cells under starvation conditions, results showed that Bortezomib significantly enhanced the proapoptotic effects of starvation. Cancer Res. 2024 Apr 1;84(7):1133-1148.
MEC2 cells 10 nM 24 h To evaluate the cytotoxic effects of Bortezomib on MEC2 cells under starvation conditions, results showed that Bortezomib significantly enhanced the proapoptotic effects of starvation. Cancer Res. 2024 Apr 1;84(7):1133-1148.
MEC1 cells 10 nM 24 h To evaluate the cytotoxic effects of Bortezomib on MEC1 cells under starvation conditions, results showed that Bortezomib significantly enhanced the proapoptotic effects of starvation. Cancer Res. 2024 Apr 1;84(7):1133-1148.
UMSCC-17A cells 0.01 –10000 nM 24 h To study the sensitivity of different HNSCC cell lines to Bortezomib, it was found that UMSCC-17A cells had a lower IC50 value for Bortezomib, indicating relative sensitivity. Cell Death Dis. 2022 Apr 9;13(4):327.
UMSCC-11 cells 0.01 –10000 nM 24 h To study the sensitivity of different HNSCC cell lines to Bortezomib, it was found that UMSCC-11 cells had a higher IC50 value for Bortezomib, indicating relative resistance. Cell Death Dis. 2022 Apr 9;13(4):327.
UMSCC-17B cells 0.01 –10000 nM 24 h To study the sensitivity of different HNSCC cell lines to Bortezomib, it was found that UMSCC-17B cells had a lower IC50 value for Bortezomib, indicating relative sensitivity. Cell Death Dis. 2022 Apr 9;13(4):327.
HN31 cells 0.01 –10000 nM 24 h To study the sensitivity of different HNSCC cell lines to Bortezomib, it was found that HN31 cells had a higher IC50 value for Bortezomib, indicating relative resistance. Cell Death Dis. 2022 Apr 9;13(4):327.
U266 cells 9.21 nM 12 h and 24 h To evaluate the inhibitory effect of anti-BCMA-Exo-Btz on myeloma cell proliferation, results showed that anti-BCMA-Exo-Btz was more effective than free Btz in suppressing myeloma cell proliferation. Blood Adv. 2024 Sep 24;8(18):4886-4899.
LP-1 cells 9.21 nM 12 h and 24 h To evaluate the inhibitory effect of anti-BCMA-Exo-Btz on myeloma cell proliferation, results showed that anti-BCMA-Exo-Btz was more effective than free Btz in suppressing myeloma cell proliferation. Blood Adv. 2024 Sep 24;8(18):4886-4899.
AMO1 cells 5 nM 24 h To evaluate the effect of ISG20L2 overexpression on BTZ sensitivity, results showed that ISG-OE AMO1 cells were less sensitive to BTZ. JCI Insight. 2022 Oct 10;7(19):e157081.
ARD cells 3.125 to 50 nM 24 h To evaluate the effect of ISG20L2 knockdown on BTZ sensitivity, results showed that ISG-KD ARD cells were more sensitive to BTZ. JCI Insight. 2022 Oct 10;7(19):e157081.
Mouse dorsal root ganglion (DRG) neurons 3 nM - 10 µM 24 h Bortezomib caused neurite retraction and neuronal death Commun Biol. 2023 Dec 5;6(1):1228.
Mouse dorsal root ganglion (DRG) neurons 100 nM 24 h Bortezomib induced long-term sensitization of TRPV1, increasing the response to capsaicin Commun Biol. 2023 Dec 5;6(1):1228.

Bortezomib/硼替佐米 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Xenograft model Subcutaneous injection 0.5 mg/kg Bortezomib every 3 days, Rom every 2 days, for 24 days Evaluate the effect of HDAC1 inhibitor Rom combined with Bortezomib, significantly suppressed tumor growth and prolonged survival Nat Commun. 2023 Mar 9;14(1):1290.
Mice GBC cell-derived xenograft (CDX) and patient-derived xenograft (PDX) animal models Intravenous injection 0.25 mg/kg Every 3 days for a total of 6 times To evaluate the antitumor efficacy of ES-NP(BTZ;Ce6) +NIR in CDX and PDX models, the results showed significant inhibition of tumor growth, with a reduction of 96.8 ± 1.5% in tumor volume. Adv Sci (Weinh). 2022 Mar;9(7):e2103895.
Mice Chronic Lymphocytic Leukemia (CLL) model Intraperitoneal injection 0.35 mg/kg Once per week for 3 weeks To evaluate the anti-CLL effects of Bortezomib in combination with Rituximab under fasting-mimicking conditions, results showed that the combination treatment significantly delayed CLL progression and prolonged mouse survival. Cancer Res. 2024 Apr 1;84(7):1133-1148.
Nude mice Subcutaneous HNSCC tumor model Tail vein injection 0.3 mg/kg Every three days for 6 weeks To study the effect of ΔNp63 α on Bortezomib resistance in vivo, it was found that silencing ΔNp63 α inhibited the growth of HN-31 cells, while forced expression of ΔNp63 α significantly promoted the growth of UMSCC-17B cells. Cell Death Dis. 2022 Apr 9;13(4):327.
NSG mice Orthotopic MM xenograft model Lateral tail vein injection 0.29 mg/kg 3 times a week for 2 weeks To evaluate the antitumor effect of anti-BCMA-Exo-Btz in vivo, results showed that anti-BCMA-Exo-Btz significantly inhibited tumor growth and prolonged the overall survival of the animals. Blood Adv. 2024 Sep 24;8(18):4886-4899.
Mice Human MM xenograft model Intraperitoneal injection 0.75 mg/kg Twice a week for 4 weeks To evaluate the effect of ISG20L2 knockdown on BTZ treatment efficacy, results showed that ISG-KD MM was more sensitive to BTZ treatment, and mice survived longer. JCI Insight. 2022 Oct 10;7(19):e157081.
Mice Wild-type and TRPV1 knockout mice Intraperitoneal injection 1 mg/kg Injected on days 1, 3, and 5, lasting for 2 weeks Bortezomib caused a reduction in intraepidermal nerve fiber density and loss of sensory function, and TRPV1 knockout mice were protected from these effects Commun Biol. 2023 Dec 5;6(1):1228.

Bortezomib/硼替佐米 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/硼替佐米 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/硼替佐米 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/硼替佐米 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/硼替佐米 技术信息

CAS号179324-69-7
分子式C19H25BN4O4
分子量 384.24
SMILES Code CC(C)C[C@@H](B(O)O)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O
MDL No. MFCD09056737
别名 PS-341; LDP-341; MLN341; MG-341; NSC 681239
运输蓝冰
InChI Key GXJABQQUPOEUTA-RDJZCZTQSA-N
Pubchem ID 387447
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
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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/硼替佐米 纯度/质量文件 | Bortezomib/硼替佐米 亚型比较 | Bortezomib/硼替佐米 生物活性 | Bortezomib/硼替佐米 动物研究 | Bortezomib/硼替佐米 临床数据 | Bortezomib/硼替佐米 参考文献 | Bortezomib/硼替佐米 实验方案 | Bortezomib/硼替佐米 技术信息

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