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Zoledronic acid (ZOL 446)
Catalog No.S1314 Synonyms: Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast
For research use only.
Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 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.
CAS No. 118072-93-8
Selleck's Zoledronic acid (ZOL 446) has been cited by 36 publications
Purity & Quality Control
Choose Selective Ras Inhibitors
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Biological Activity
| Description | Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 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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| Targets |
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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] |
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| Cell Data |
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| Assay |
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| 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] |
Protocol (from reference)
Solubility (25°C)
|
In vitro |
0.1M NaOH (aq) |
40 mg/mL
(147.01 mM) |
| DMSO |
0.004 mg/mL
(0.01 mM) |
|
| Water |
Insoluble
|
Chemical Information
| Molecular Weight | 272.09 | ||
|---|---|---|---|
| Formula | C5H10N2O7P2 |
||
| CAS No. | 118072-93-8 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05080790 | Recruiting | Drug: Dinutuximab Beta Zoledronic acid Interleukin-2 | Leiomyosarcoma | Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest|EUSA Pharma Inc. | November 15 2021 | Phase 2 |
| NCT04719481 | Not yet recruiting | Drug: Pravastatin Sodium 80 MG|Drug: Placebo | Postmenopausal Osteoporosis | Peking University Third Hospital | November 2021 | Phase 4 |
| NCT04719650 | Not yet recruiting | Drug: Zoledronic Acid Injection|Drug: Placebo | Postmenopausal Osteoporosis | Peking University Third Hospital | October 2021 | Phase 4 |
| NCT04034199 | Unknown status | Drug: Denosumab|Drug: Zoledronic Acid | Idiopathic Inflammatory Myopathies|Osteoporosis Osteopenia | Kwong Wah Hospital|Tung Wah Group of Hospitals | August 15 2019 | Phase 3 |
| NCT03862833 | Recruiting | Drug: IL2|Drug: Zoledronic Acid | Hematopoietic Stem Cell Transplantation | Nantes University Hospital | May 7 2019 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Question 1:
How can I reconstitute the compound for in vivo studies?
Answer:
Please dissolve this compound directly to 30% PEG400+0.5% Tween80+5% Propylene glycol.
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