Zoledronic acid monohydrate

For research use only.

Catalog No.S5244 Synonyms: zoledronate monohydrate, CGP-4244 monohydrate

5 publications

Zoledronic acid monohydrate Chemical Structure

CAS No. 165800-06-6

Zoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which 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.

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Selleck's Zoledronic acid monohydrate has been cited by 5 publications

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Description Zoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which 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.
Ras [1]
Rho [1]
In vitro

Zoledronic acid inhibits osteoclast maturation indirectly by increasing OPG protein secretion and decreasing transmembrane RANKL expression in human osteoblasts. Treatment of primary human OB‐like cells with the potent nitrogen-containing BP, zoledronic acid (ZOL), resulted in a downregulation of membrane-ssociated RANKL protein expression. In addition to direct effects on cells of the osteoclast lineage, zoledronic acid may inhibit bone resorption by reducing transmembrane RANKL expression and increasing OPG secretion in osteoclast (OB)-like cells[1]. Zoledronic acid induces growth inhibition (IC50:10–50 μM) and apoptotic death of human pancreatic cancer cells. The proapoptotic effect was correlated to cleavage/activation of caspase-9 and poly(ADP)-ribose polymerase, but not of caspase-3. It interferes with growth and survival pathways downstream to p21ras[2]. Zoledronic acid is also a potent inhibitor of angiogenesis. In vitro, zoledronic acid inhibits proliferation of human endothelial cells stimulated with fetal calf serum, basic fibroblast growth factor (bFGF), and vascular endothelial growth factor (IC50 values 4.1, 4.2, and 6.9 μM, respectively), and modulates endothelial cell adhesion and migration. In cultured aortic rings and in the chicken egg chorioallantoic membrane assay, zoledronic acid reduces vessel sprouting. ZOL also exerted a concentration-dependent, biphasic effect on the adhesion and migration of HUVEC in vitro. ZOL concentrations of 1 and 3 μM increased cell adhesion but inhibited it at 30 and 100 μM. Similarly, cell migration was stimulated by 0.3 to 10 μM ZOL, whereas 30 μM completely inhibited it. These findings suggest that ZOL could interfere with cytoskeletal function in endothelial cells[4].

In vivo Zoledronic acid affects breast cancer metastasis to visceral organs as well as bone[3]. When administered systemically to mice, zoledronic acid potently inhibits the angiogenesis induced by subcutaneous implants impregnated with bFGF [ED50, 3 μg/kg (7.5 nmol/kg) s.c.][4]. In nice transplanted with osteosarcoma (OS) cells, ZOL administration prevented osteolysis and significantly reduced the amount of OS-induced bone formation while has no effect on tumor burden at the primary site. ZOL failed to reduce lung metastasis and in some cases was associated with larger and more numerous metastatic lesions[5].


Cell Research:


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  • Cell lines: human PC cell lines (BxPC-3, CFPAC-1 and PANC-1)
  • Concentrations: 1-100 μM
  • Incubation Time: 72 h
  • Method:

    'BxPC-3 and CFPAC-1 are adherent human pancreatic adenocarcinoma cell lines that were grown in RPMI 1640 and Iscove's modified Dulbecco's media, respectively. PANC-1 is a human epithelioid pancreas carcinoma cell line that was grown in Dulbecco's modified Eagle's medium (DMEM). All media were supplemented with 10% heat-inactivated fetal bovine serum, 2 mM L-glutamine, 100 μg/ml streptomycin and 100 U/ml penicillin. All PC cell lines were cultured at a constant temperature of 37°C in a humidified atmosphere of 5% carbon dioxide (CO2). The neutralised sodium salt of ZOL was dissolved in sterile ddH2O and used at a final concentration in a range of 1-100 μM. Analysis of cell proliferation was performed on PC cells in the presence of increasing concentrations of ZOL by the MTT assay. Briefly, PC cells (3 × 104/well) were seeded in 96-well plates in serum-containing media and allowed to attach for 24 h. The medium was then removed and replaced with new medium containing ZOL at different concentrations. Cells were incubated under these conditions for a time course spanning 72 h. Then cells were incubated with 10 μl well−1 of thiazolyl blue (MTT, 5 mg/ml) for 1 h at 37°C. After incubation, 100 μl of 0.04 N HCl in isopropanol was added into each well and the absorbance was measured at a wavelength of 620 nm in a microplate reader.

    (Only for Reference)
Animal Research:


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  • Animal Models: Female mice (strain Tiflbm:MAG)
  • Dosages: 1, 10 and 100 μg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.01 mg/mL (0.03 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 290.1


CAS No. 165800-06-6
Storage powder
in solvent
Synonyms zoledronate monohydrate, CGP-4244 monohydrate
Smiles C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O.O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04034199 Not yet recruiting 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
NCT03301285 Completed Drug: Zoledronic Acid Multiple Disability|Osteoporosis Central Hospital Nancy France January 1 2017 --
NCT02632903 Withdrawn Drug: Zoledronic acid Osteoporosis|Osteonecrosis|Acute Lymphoblastic Leukemia Children''s Hospital of Eastern Ontario October 2016 Phase 2

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Ras Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID