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受注：045-509-1970 |
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化学情報
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Synonyms | LDP-341, MLM341, NSC 681239,PS-341, BTZ | Storage (From the date of receipt) |
3 years-20°C （in the dark）powder | |||
| 化学式 | C19H25BN4O4 |
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| 分子量 | 384.24 | CAS No. | 179324-69-7 | ||||
| Solubility (25°C)* | 体外 | DMSO | 76 mg/mL (197.79 mM) | ||||
| Water | Insoluble | ||||||
| Ethanol | Insoluble | ||||||
| 体内 （毎回新しく調製した物を用意してください） |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。 |
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| in vitro | Bortezomib, a boronic acid dipeptide, is a highly selective, reversible inhibitor of the 26S proteasome which primarily functions in the degradation of mis-folded proteins and is essential for the regulation of the cell cycle. Exposure to this compound has been shown to stabilize p21, p27, and p53, as well as the proapoptotic Bid and Bax proteins, caveolin-1, and inhibitor κB-α, which prevents activation of nuclear factor κB-induced cell survival pathways. It also promotes the activation of the proapoptotic c-Jun-NH2 terminal kinase, as well as the endoplasmic reticulum stress response. Alteration of the levels of these cellular proteins leads to inhibition of proliferation, migration, and promotion of apoptosis of cancer cells. [2] This chemical is shown to penetrate into cells and inhibit proteasome-mediated intracellular proteolysis of long-lived proteins with a concentration that inhibits 50% of the proteolysis of ∼0.1 μM. The average growth inhibition of 50% value for this compound across the entire panel of 60 cancer cell lines derived from multiple human tumors from the US National Cancer Institute (NCI) is 7 nM. Treatment of PC-3 cells with it (100 nM) for 8 h results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. It kills PC-3 cells at 24 and 48 hr with IC50 of 100 and 20 nM, respectively. This agent induces nuclear condensation at 16–24 hr after treatment. Its treatment leads to PARP cleavage in a time-dependent manner with concentrations as low as 100 nM being effective at 24 hr. [1] |
| in vivo | The anticancer effects of bortezomib as a single agent have been demonstrated in xenograft models of multiple myeloma, adult T-cell leukemia, lung, breast, prostate, pancreatic, head and neck, and colon cancer, and in melanoma. [2] Oral administration of this compound at 1.0 mg/ kg daily for 18 days causes tumor growth delays, as well as a decrease in the number of metastases in the Lewis lung cancer model. This compound at a single dose of up to 5 mg/kg significantly decreased the surviving fraction of breast tumor cells. Administration of this chemical weekly at 1.0 mg/kg for 4 weeks reduces tumor growth by 60% in murine xenograft models of prostate cancer. Treatment with this agent at 1.0 mg/kg for 4 weeks results in a 72% or 84% reduction in pancreatic cancer murine xenografts growth, as well as an increase in tumor cell apoptosis. This compound at 1.0 mg/kg results in significant inhibition of human plasmacytoma xenograft growth, increase in tumor cells apoptosis and overall survival, and a decrease in tumor angiogenesis. [3] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Kinetic Methods | |
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| In a typical kinetic run, 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) and Suc-Leu-Leu-Val-Tyr-AMC in DMSO are added to a 3 mL fluorescence cuvette, and the cuvette is placed in the jacketed cell holder of a fluorescence spectrophotometer. Reaction temperature is maintained at 37℃ by a circulating water bath. After the reaction solution has reached thermal equilibrium (5 minutes), 1 μL−10 μL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (λex= 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates. | ||
| 細胞アッセイ | 細胞株 | Human multiple myeloma cells line U266 |
| 濃度 | ~10 μM | |
| 反応時間 | 2 days | |
| 実験の流れ | The inhibitory effect of Bortezomib on cell growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-hour cultures are pulsed with 10 μL of 5 mg/mL MTT to each well for the last 4 hour of 48-hour cultures, followed by 100 μL of isopropanol containing 0.04 N HCl. Absorbance is measured at 570 nm using a spectrophotometer. |
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| 動物実験 | 動物モデル | Human plasmacytoma xenografts RPMI 8226 |
| 投薬量 | 1 mg/kg | |
| 投与方法 | i.v. twice weekly for 4 weeks, then once weekly | |
参考
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カスタマーフィードバック
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Data from [Data independently produced by Sci Transl Med, 2015, 6(250), 250ra112]
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Data from [Data independently produced by Cancer Res, 2015, 75(8), 1714-24]
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Data from [Data independently produced by J Clin Invest, 2014, 124(9), 3757-66]
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| Bone Marrow-Targeted Liposomes Loaded with Bortezomib Overcome Multiple Myeloma Resistance [ ACS Nano, 2025, 19(12):11684-11701] | PubMed: 40117329 |
| USP7 V517F mutation as a mechanism of inhibitor resistance [ Nat Commun, 2025, 16(1):2526] | PubMed: 40087304 |
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| Microbiota-derived urolithin A in monoclonal gammopathies and multiple myeloma therapy [ Microbiome, 2025, 13(1):56] | PubMed: 40022244 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。