受注:045-509-1970 |
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Synonyms | ZA, CGP-4244, GP42446A, ZOL 446 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C5H10N2O7P2 |
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分子量 | 272.09 | CAS No. | 118072-93-8 | |
Solubility (25°C)* | 体外 | 0.5MNAOH | 6.05 mg/mL (22.23 mM) | |
DMSO | 0.005 mg/mL (0.01 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Zoledronic acid (Zoledronate), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy. |
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in vitro | Zoledronic acid (10 µM and 100 µM) causes a significant reduction in the proportions of MCF-7 cells (49.54% and 23.55% of control, respectively) (P < 0.05). Zoledronic acid has little effect on MDA-MB-231 cells at concentrations of 0.1–10 µM, whereas the 100 µM concentration results in a significant reduction in cell number. Zoledronic acid (100 µM) results in a 63.5% reduction in MCF-7 cell number at 72 hours and an 87.1% reduction at 96 hours. Zoledronic acid (10 µM) results in a greater than 4-fold increase in MCF-7 cell apoptosis whereas the 100 µM concentration induces a 6-fold increase in the proportion of apoptotic cells. Zoledronic acid (10 µM) and paclitaxel (2 µM) results in a 5-fold increase in apoptosis (774.8% of control) compared to zoledronic acid alone (155.71%) and a 4-fold increase compared to paclitaxel alone (189.68%). Zoledronic acid-induced apoptosis of MCF-7 breast cancer cells can be inhibited by addition of intermediates of the mevalonate pathway, which is consistent with observations in osteoclasts, macrophages and myeloma cells. [1] Zoledronic acid enhances OPG gene expression and protein secretion by human osteoblasts (hOB) in a dose-dependent fashion with a maximum effect at 10 nM after 72 hours, consistent with the higher biological potency of Zoledronic acid. Zoledronic acid prevents the inhibitory effects of the glucocorticoid dexamethasone on OPG mRNA and protein production in human osteoblasts. Zoledronic acid induces type I collagen secretion and alkaline phosphatase activity by 2- and 4-fold, respectively, in human osteoblasts. [2] |
in vivo | Zoledronic acid (120 mg/kg, s.c.) prevents the formation of lesions, prevents cancellous bone loss and loss of bone mineral density, and reduces osteoclast perimeter in 5T2MM-bearing mice. Zoledronic acid (120 mg/kg, s.c.) also decreases paraprotein concentration, decreases tumor burden, and reduces angiogenesis in 5T2MM-bearing mice. [3] |
細胞アッセイ | 細胞株 | MCF7 cells |
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濃度 | 100 μM | |
反応時間 | 72 h | |
実験の流れ | Cells were treated with various concentrations of drug for 72 h. |
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動物実験 | 動物モデル | Male C57BL/KaLwRij mice |
投薬量 | 120 µg/kg | |
投与方法 | s.c. |
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Data from [Data independently produced by Liver Int, 2013, 33(1), 127-36]
Data from [Data independently produced by , , J Mol Cell Cardiol, 2016, 99:76-86.]
BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism [ Nat Commun, 2023, 14(1):1413] | PubMed: 36918560 |
BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism [ Nature Communications, 2023, 1413-2023)] | PubMed: None |
Priming of Colorectal Tumor-Associated Fibroblasts with Zoledronic Acid Conjugated to the Anti-Epidermal Growth Factor Receptor Antibody Cetuximab Elicits Anti-Tumor Vδ2 T Lymphocytes [ Cancers (Basel), 2023, 15(3)610] | PubMed: 36765569 |
Priming of Colorectal Tumor-Associated Fibroblasts with Zoledronic Acid Conjugated to the Anti-Epidermal Growth Factor Receptor Antibody Cetuximab Elicits Anti-Tumor Vδ2 T Lymphocytes [ Cancers (Basel), 2023, 15(3)610] | PubMed: 36765569 |
γδ-Enriched CAR-T cell therapy for bone metastatic castrate-resistant prostate cancer [ Sci Adv, 2023, 9(18):eadf0108] | PubMed: 37134157 |
Select HDAC Inhibitors Enhance Osteolysis and Bone Metastasis Outgrowth but Can Be Mitigated With Bisphosphonate Therapy [ JBMR Plus, 2023, 7(3):e10694] | PubMed: 36936362 |
Zoledronic Acid Inhibits the Growth of Breast Malignant Phyllodes Tumor by Inducing Mitotic Catastrophe Via the Plk1 Signaling Pathway [ SSRN, 2023, 38 Pages] | PubMed: none |
Targeting of colorectal cancer organoids with zoledronic acid conjugated to the anti-EGFR antibody cetuximab [ J Immunother Cancer, 2022, 10(12)e005660] | PubMed: 36543375 |
Label-free metabolic imaging for sensitive and robust monitoring of anti-CD47 immunotherapy response in triple-negative breast cancer [ J Immunother Cancer, 2022, 10-9e005199] | PubMed: 36096527 |
Label-free metabolic imaging for sensitive and robust monitoring of anti-CD47 immunotherapy response in triple-negative breast cancer [ J Immunother Cancer, 2022, 10-9e005199] | PubMed: 36096527 |
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。