Zoledronic Acid |
| Catalog No.GC14701 |
Potent nitrogen-containing bisphosphonates
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118072-93-8
Sample solution is provided at 25 µL, 10mM.
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Zoledronic Acid is a third-generation, nitrogen-containing bisphosphonate, inhibits osteoclast-mediated bone resorption, and also has antitumor activity.
Zoledronic Acid induces apoptosis in HGF and HaCaT cells at 0.5 μM, and causes cell death at 1-5 μM[1]. Zoledronic Acid (50, 100 μM) causes dose- and time-dependent apoptosis in CNE-2Z cells after treatment for 24, 48, and 72 h. Zoledronic Acid (50 μM) also increases the level of ROS, which is supposed to mediate Cl- currents activation in CNE-2Z cells. Furthermore, the apoptosis and chloride currents induced by Zoledronic Acid can be blocked by knocking down ClC-3 protein expression[2].
References:
[1]. Scheper M, et al. A novel soft-tissue in vitro model for bisphosphonate-associated osteonecrosis. ibrogenesis Tissue Repair. 2010 Apr 1;3:6.
[2]. Wang L, et al. The apoptotic effect of Zoledronic acid on the nasopharyngeal carcinoma cells via ROS mediated chloride channel activation. Clin Exp Pharmacol Physiol. 2018 Jun 8.
| Cell experiment [1]: | |
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Cell lines |
The human breast carcinoma cell lines (MCF-7 and MDA-MB-231) |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1–100 μM for 72 hours. |
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Applications |
Treatment of MCF-7 cells with a range of zoledronic acid concentrations had little effect on apoptosis at 0.1 and 1.0 μM, however, an increase in the proportion of apoptotic cells was observed with 10 μM and 100 μM zoledronic acid compared with control (28.7% and 70.7% vs 22.57%, respectively).Treatment of MDA-MB-231 cells with 0.1–1 μM zoledronic acid did not cause an increase in apoptosis, but treatment with the 10 and 100 μM zoledronic acid resulted in a significant increase in the proportions of apoptotic cells (126.6% and 126.6% of control). A significant time-dependent increase in MCF7 cell apoptosis was confirmed when cells were incubated with 100 μM zoledronic acid for 24–96 hours. |
| Animal experiment [2]: | |
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Animal models |
The 5T2MM murine model (Male, 6-week-old, C57BL/KaLwRijHsd mice) |
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Dosage form |
120 g/kg, subcutaneously (sc), twice weekly, 12 weeks. |
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Application |
Treatment of mice bearing 5T2MM cells with zoledronic acid clearly prevented the development of osteolytic bone disease, decreased tumor burden in bone, and increased survival in a model of established myeloma. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Jagdev SP, Coleman RE, Shipman CM , et al .The bisphosphonate, zoledronic acid, induces apoptosis of breast cancer cells: evidence for synergy with paclitaxel. Br J Cancer. 2001 Apr 20;84(8):1126-34. [2] Croucher PI, De Hendrik R, Perry MJ, et al. Zoledronic Acid Treatment of 5T2MM-Bearing Mice Inhibits the Development of Myeloma Bone Disease: Evidence for Decreased Osteolysis, Tumor Burden and Angiogenesis, and Increased Survival .J Bone Miner Res. 2003 Mar;18(3):482-92 | |
| Cas No. | 118072-93-8 | SDF | |
| Chemical Name | (1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid | ||
| Canonical SMILES | C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O | ||
| Formula | C5H10N2O7P2 | M.Wt | 272.09 |
| Solubility | ≥ 6.8mg/mL in Water with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6753 mL | 18.3763 mL | 36.7525 mL |
| 5 mM | 735.1 μL | 3.6753 mL | 7.3505 mL |
| 10 mM | 367.5 μL | 1.8376 mL | 3.6753 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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