Zoledronic Acid

For research use only.

Catalog No.S1314 Synonyms: Zoledronate, CGP-4244

19 publications

Zoledronic Acid  Chemical Structure

Molecular Weight(MW): 272.09

Zoledronic acid (ZA), 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.

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Selleck's Zoledronic Acid has been cited by 19 publications

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Biological Activity

Description Zoledronic acid (ZA), 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.
Rho [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human foreskin fibroblast monolayer cells (HFF cells) MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH;lRpZKdiC4aYTyc{BqdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDD0bIUh\3Kxd4ToJI9nKFSxeH;wcIF{dWFiZ3;u[IlqKGmwIHj1cYFvKG[xcnXzb4lvKG[rYoLvZoxie3RibX;uc4xigWW{IHPlcIx{KCiKRl[gZ4VtdHNrLDDJR|UxRTBwN{mg{txO NE\qUWsyPTh3N{GxPS=>
human Gamma delta T cells MXHGeY5kfGmxbjDhd5NigQ>? MWHF[oZm[3SrdnWgZ49v[2WwdILheIlwdiCjZ3HpcpN1KGi3bXHuJGdidW2jIHTlcJRiKFRiY3XscJMtKEWFNUC9OU41KM7:TR?= M1\wRVE2QDJ6OEO0
mouse J774 cells NU[4ephxS3m2b4TvfIlkyqCjc4PhfS=> M3rkO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGo4PzRiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7LDDJR|UxRTdwODFOwG0> MWeyOFgyOzd2Mh?=
human RPMI8226 cells M1y5W2N6fG:2b4jpZ:Kh[XO|YYm= MnK3O|IhcA>? Ml\OR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnBOUTh{Mk[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiRVO1NF0yOSEQvF2= MYSyN|k6QDl{MR?=
human NCI-H460 cell M2HJfnBzd2yrZnXyZZRqd25iYYPzZZk> Mof6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsJIxqdmViYomgUXRVKGG|c3H5MEBKSzVyPUGxMlch|ryP NGfIcYgyPjl5MESwOS=>
human SF-268 cell M1e4S3Bzd2yrZnXyZZRqd25iYYPzZZk> M{C4VWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[tNlY5KGOnbHygcIlv\SCkeTDNWHQh[XO|YYmsJGlEPTB;MUSuN{DPxE1? M4X6RVE3QTdyNEC1
human MCF7 cells NWfMdFgzWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFTrSog4OiCq M33NZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTJ|IN88US=> MkLxNlQ6Ojh|OUm=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
ALDH1 / Oct4 / Nanog / Sox2 / CD49f ; 

PubMed: 30791957     

Western blot analysis of ALDH1, Sox2, CD49f, Nanog, and Oct4 in cervical cancer cells derived CSCs treated or not with zoledronic acid (10, 20, and 30 μM).

N-cadherin / E-cadherin / Vimentin ; 

PubMed: 30791957     

Western blot analysis of E-cadherin, N-cadherin, and Vimentin in cervical cancer cells derived CSCs treated or not with zoledronic acid (10, 20, and 30 μM).

Growth inhibition assay
Cell viability; 

PubMed: 30791957     

Zoledronic acid inhibits the proliferation of cervical cancer cells derived CSCs in vitro. Parental HeLa, SiHa, and CaSki cells as well as their derived CSCs were seeded in 96-well plates and treated with zoledronic acid at different concentrations for 1–5 days. Cell viability was determined by the modified MTT assay. OD values of each treated group were compared with that of the control at the same time point. Control vs. 5, 10, 20, 40, and 80 μM of zoledronic acid: * P < 0.05, ** P < 0.01. Results are shown as mean values ± SD of independent experiments performed in triplicate.

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]


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

* 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 272.09


CAS No. 118072-93-8
Storage powder
in solvent
Synonyms Zoledronate, CGP-4244

In vivo Formulation Calculator (Clear solution)

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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

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.

Handling Instructions

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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.

Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID