Bortezomib

カタログ番号 T2399 CAS 179324-69-7

別名: Radiciol, NSC 681239, MG 341, DPBA, Brotezamide, LDP 341

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.

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Bortezomib, CAS 179324-69-7

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
5 mg	在庫あり	￥ 11,000
10 mg	在庫あり	￥ 13,500
25 mg	在庫あり	￥ 17,000
50 mg	在庫あり	￥ 20,500
100 mg	在庫あり	￥ 34,000
200 mg	在庫あり	￥ 54,500
500 mg	在庫あり	￥ 90,000
1 mL * 10 mM (in DMSO)	在庫あり	￥ 11,000

バルクのお問い合わせ

バッチを選択

純度: 100%

COA DATASHEET SDS LCMS HNMR

純度: 99.91%

DATASHEET SDS

純度: 99.91%

COA DATASHEET SDS HPLC

純度: 99.59%

COA DATASHEET SDS HNMR HPLC

純度: 98%

COA DATASHEET SDS HNMR

COA DATASHEET SDS

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	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.
ターゲット＆IC50	20S proteasome:0.6 nM (cell free)
In vitro	METHODS: Human tongue squamous carcinoma cells SCC-15 and CAL-27, human pharyngeal squamous carcinoma cells FaDu, and human salivary gland carcinoma cells A-253 and SALTO-5 were treated with Bortezomib (6.25-100 nM) for 24-72 h. The growth inhibition of these cells was detected by SRB. RESULTS: The effects of Bortezomib on the proliferation of the five tumor cells were dose- and time-dependent, and SCC-15 was the most sensitive cell to the effects of Bortezomib. SCC-15 was the most sensitive cell to the effect of Bortezomib.[1] METHODS: Human small cell lung cancer cells NCI-H69 and NCI-H2171 were treated with Bortezomib (0.05 μM; 0.5 μM) for 48 h. Cell cycle and apoptosis were detected by Flow Cytometry. RESULTS: Bortezomib induced cell cycle arrest in the G2-M transition state, increased the number of G2-phase cells and decreased the number of S-phase cells, and induced apoptosis in tumor cells. [2] METHODS: H460, a large cell lung cancer cell, was incubated with Bortezomib (0.01-10 μM) for 3-48 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Bortezomib treatment resulted in concentration-dependent phosphorylation of Bcl-2 protein. Starting at 12 h, a recognizable Bcl-2 cleavage product was observed, and Bcl-2 phosphorylation preceded Bcl-2 cleavage for at least 9 h.[3]
In vivo	METHODS: To detect anti-tumor activity in vivo, Bortezomib (0.3 mg/kg) was administered intraperitoneally to NOD/SCID mice bearing primary exudative lymphoma (PEL) UM-PEL-1 once daily for three weeks. RESULTS: Bortezomib induced remission of PEL and prolonged overall survival of mice with lymphoma exudates. bortezomib downregulated cell cycle progression, DNA replication, and Myc target genes. [4] METHODS: To investigate the effect of Bortezomib on renal fibrosis, Bortezomib (0.5 mg/kg) was intraperitoneally injected into an aristolochic acid I (AA)-induced fibrotic C57BL/6J mouse model twice a week for ten weeks. RESULTS: Bortezomib treatment significantly attenuated AA-induced renal dysfunction and proteinuria, reduced the expression of renal fibrosis-associated proteins and markers of renal injury, such as αSMA, Kim1, and Ngal, and prevented renal fibrosis at histopathologic level. [5]
キナーゼ試験	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].
細胞研究	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].
動物実験	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].

別名	Radiciol, NSC 681239, MG 341, DPBA, Brotezamide, LDP 341
分子量	384.24
分子式	C19H25BN4O4
CAS No.	179324-69-7

保存条件

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

H2O: Insoluble

Ethanol: Insoluble

DMSO: 71 mg/mL (184.8 mM)

参考文献

1. Benvenuto M, et al. Proteasome inhibition by bortezomib parallels a reduction in head and neck cancer cells growth, and an increase in tumor-infiltrating immune cells. Sci Rep. 2021 Sep 24;11(1):19051. 2. Taromi S, et al. Proteasome inhibitor bortezomib enhances the effect of standard chemotherapy in small cell lung cancer. Oncotarget. 2017 Sep 23;8(57):97061-97078. 3. Ling YH, 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 Aug;1(10):841-9. 4. Sarosiek KA, et al. Efficacy of bortezomib in a direct xenograft model of primary effusion lymphoma. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13069-74. 5. Zeniya M, et al. The proteasome inhibitor bortezomib attenuates renal fibrosis in mice via the suppression of TGF-β1. Sci Rep. 2017 Oct 12;7(1):13086. 6. Qu, Yuan Qing, et al. 2-Aminoethoxydiphenylborane sensitizes anti-tumor effect of bortezomib via suppression of calcium-mediated autophagy. Cell death & disease. 2018 Mar 2;9(3):361.

引用文献

1. Zhou Q, Liang J, Yang T, et al. Carfilzomib modulates tumor microenvironment to potentiate immune checkpoint therapy for cancer. EMBO Molecular Medicine. 2022 Jan 11;14(1):e14502. doi: 10.15252/emmm.202114502. Epub 2021 Dec 13. 2. Li Q, Chu Y, Li S, et al. The oncoprotein MUC1 facilitates breast cancer progression by promoting Pink1-dependent mitophagy via ATAD3A destabilization. Cell Death & Disease. 2022, 13(10): 1-16. 3. Qu, Yuan Qing, et al. 2-Aminoethoxydiphenylborane sensitizes anti-tumor effect of bortezomib via suppression of calcium-mediated autophagy. Cell Death & Disease. 2018, 9(3): 1-15 4. Zhang L, Xu L, Zhang X, et al. Methyltransferase Setdb1 Promotes Osteoblast Proliferation by Epigenetically Silencing Macrod2 with the Assistance of Atf7ip. Cells. 2022, 11(16): 2580. 5. Chen X, Chen Y, Ou Y, et al. Bortezomib inhibits NLRP3 inflammasome activation and NF-κB pathway to reduce psoriatic inflammation. Biochemical Pharmacology. 2022, 206: 115326. 6. Liu M, Zhao Y T, Lv Y Y, et al. Metformin Relieves Bortezomib-Induced Neuropathic Pain by Regulating AMPKa2-Mediated Autophagy in the Spinal Dorsal Horn. Neurochemical Research. 2022: 1-10. 7. Sassetti E, Durante Cruz C, Identification and Characterization of Approved Drugs and Drug-Like Compounds as Covalent Escherichia coli ClpP Inhibitors. International Journal of Molecular Sciences. 2019, 20(11): 2686 8. Wang M, Wang J, Tsui A Y P, et al. Mechanisms of peripheral neurotoxicity associated with four chemotherapy drugs using human induced pluripotent stem cell-derived peripheral neurons. Toxicology in Vitro. 2021: 105233. 9. Liang Y, Qian Y, Tang J, et al.Arsenic trioxide promotes ERK1/2-mediated phosphorylation and degradation of BIMEL to attenuate apoptosis in BEAS-2B cells.Chemico-Biological Interactions.2022: 110304. 10. He Y, Shi Q, Ling Y, et al.ABLIM1, a novel ubiquitin E3 ligase, promotes growth and metastasis of colorectal cancer through targeting IĸBα ubiquitination and activating NF-ĸB signaling.Cell Death & Differentiation.2024: 1-14.

11. Zhang H, Wang H, Hu Y, et al.Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma.Cancer Letters.2024: 216802.

もっと見る隠し

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Bortezomib 179324-69-7 Apoptosis Autophagy NF-Κb Proteases/Proteasome Ubiquitination Proteasome NF-κB Nuclear factor-kappaB Inhibitor LDP-341 Nuclear factor-κB LDP341 PS 341 PS341 Radiciol MG341 PS-341 NSC 681239 inhibit MG 341 DPBA NSC-681239 NSC681239 Brotezamide LDP 341 MG-341 inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Bortezomib

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords