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Zoledronic acid (Zoledronate)

Name: Zoledronic acid (Zoledronate)
Brand: Selleck Chemicals
SKU: S1314
Rating: 5 (54 reviews)

Synonyms: ZA, CGP-4244, GP42446A, ZOL 446

Catalog No.S1314 Purity:99.80%

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.

Zoledronic acid (Zoledronate) Chemical Structure

CAS No. 118072-93-8

Purity & Quality Control

Batch: Purity: 99.80%

99.80

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Signaling Pathway

Ras Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human NCI-H460 cell	Proliferation assay			Antiproliferative activity against human NCI-H460 cell line by MTT assay, IC50=11.7 μM	16970405
human SF-268 cell	Proliferation assay			Antiproliferative activity against human SF-268 cell line by MTT assay, IC50=14.3 μM	16970405
Gamma delta T cells	Function assay			Effective concentration against human Gamma delta T cells, EC50=5.4μM	15828834
HFF cells	Function assay			In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells), IC50=0.79μM	15857119
HFF cells	Function assay			Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 0.60 uM, experiment 1), IC50=7.8μM	15857119
HFF cells	Function assay			Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 0.79 uM, experiment 3), IC50=7.8μM	15857119
HFF cells	Function assay			Inhibitory concentration against the growth of Toxoplasma gondii overexpressing FPPS enzyme in human foreskin fibroblast monolayer cells; (control = 1.1 uM, experiment 2), IC50=8.3μM	15857119
BT-549	Antitumor assay			Antitumor activity against human BT-549 cells xenografted SCID mouse co-transfected with human gamma delta T lymphocytes assessed as survival time prolongation at 2 ug, ip coadministered with human recombinant IL2	18937434
BT-549	Antitumor assay			Antitumor activity against human BT-549 cells xenografted SCID mouse co-transfected with human gamma delta T lymphocytes assessed as survival time prolongation at 5 ug, ip coadministered with human recombinant IL2	18937434
BL21(DE3)	Function assay		30 mins	Inhibition of His6-tagged human truncated FPPS (6-353) expressed in Escherichia coli BL21(DE3) cells using geranyl diphosphate and isopentenyl diphosphate as substrate preincubated with enzyme for 30 mins by spectrophotometric analysis, IC50=0.1μM	23610597
BL2-codon plus (DE3) RIL	Function assay		30 mins	Inhibition of N-terminal His6-tagged Plasmodium vivax GGPPS expressed in Escherichia coli BL2-codon plus (DE3) RIL cells using geranyl diphosphate and isopentenyl diphosphate as substrate preincubated with enzyme for 30 mins by spectrophotometric analysis, IC50=0.13μM	23610597
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay, EC50=11μM	23998921
J774	Cytotoxicity assay			Cytotoxicity against mouse J774 cells assessed as reduction in cell viability, IC50=7.8μM	24813742
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=23μM	24928399
Vgamma9/Vdelta2 T-cells	Function assay		18 hrs	Binding affinity to butyrophilin 3A1 in human Vgamma9/Vdelta2 T-cells assessed as activation of Vgamma9/Vdelta2 T-cells by upregulation of CD69 and CD25 after 18 hrs, EC50=0.4866μM	29457898
RPMI8226	Antiproliferative assay		72 hrs	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay, EC50=11μM	30016091
RPMI8226	Function assay	0.5 uM		Inhibition of GGPPS in human RPMI8226 cells assessed as reduction in Rap1A prenylation at 0.5 uM by Western blot analysis	30016091
J774A.1	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against mouse J774A.1 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
RAW264.7	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
MG63	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against human MG63 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
PC3	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability at 100 uM after 72 hrs by WST8 assay	30216851
RAW264.7	Antiproliferative assay	100 uM	72 hrs	Antiproliferative activity against RANKL-differentiated mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by CCK8 assay	30216851
RAW264.7	Function assay		72 hrs	Inhibition of RANKL-induced osteoclastogenesis in mouse RAW264.7 cells after 72 hrs by TRAP staining based microscopic analysis	30216851
MC3T3-E1	Function assay	30 to 50 nM	10 to 15 days	Induction of mineralization in mouse MC3T3-E1 cells at 30 to 50 nM after 10 to 15 days by alizarin red dye based assay	30216851
C57BL mouse bone marrow cells	Function assay	50 nM	10 to 15 days	Induction of mineralization in C57BL mouse bone marrow cells at 50 nM supplemented with fresh medium containing compound every 3 days for 10 to 15 days by alizarin red dye based assay	30216851
C57BL mouse bone marrow cells/human PC3 cells	Function assay	50 to 100 nM	10 to 15 days	Induction of mineralization in C57BL mouse bone marrow cells co-cultured with human PC3 cells at 50 to 100 nM supplemented with fresh medium containing compound every 3 days for 10 to 15 days by alizarin red dye based assay	30216851
K562	Function assay		240 mins	Activation of butyrophilin 3A1 in human K562 cells assessed as interferon-gamma production pretreated for 240 mins followed by HMBPP-treated Vgamma9Vdelta2 T cells addition and measured after 20 hrs by ELISA, EC50=23μM	31531198
MIAPaCa2	Cytotoxicity assay		72 hrs	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay, EC50=13.4μM	31725297
PANC1	Cytotoxicity assay		72 hrs	Cytotoxicity against human PANC1 cells assessed as decrease in cell growth measured after 72 hrs by MTT assay, EC50=16.1μM	31725297
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

Rho ^[1]
(Cell-free assay)

Ras ^[1]

In vitro
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 Research	Cell lines	MCF7 cells
	Concentrations	100 μM
	Incubation Time	72 h
	Method	Cells were treated with various concentrations of drug for 72 h.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	ALDH1 / Oct4 / Nanog / Sox2 / CD49f N-cadherin / E-cadherin / Vimentin		30791957
	Growth inhibition assay	Cell viability		30791957

In Vivo
In vivo	Zoledronic acid (120 ug/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]
Animal Research	Animal Models	Male C57BL/KaLwRij mice
	Dosages	120 µg/kg
	Administration	s.c.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06217718	Not yet recruiting	Copd\|Empowerment\|Empowerment Patient\|Self Efficacy	Zahide Aksoy\|The Scientific and Technological Research Council of Turkey\|Marmara University	February 15 2024	Not Applicable
NCT05743179	Recruiting	Hip Fractures\|Pneumonia	The University of Hong Kong\|Queen Mary Hospital Hong Kong\|Caritas Medical Centre Hong Kong\|Prince of Wales Hospital Shatin Hong Kong\|United Christian Hospital	December 5 2022	Phase 4
NCT02864784	Withdrawn	Castrate Resistant Prostate Cancer With Bone Metastasis	Amorphical Ltd.	June 2022	Phase 1
NCT04957641	Completed	Hereditary Angioedema	Takeda	April 21 2022	--
NCT05213286	Unknown status	Autism Spectrum Disorder\|Schizotypal Disorder	Glostrup University Hospital Copenhagen	February 1 2022	Not Applicable

References

Chemical Information & Solubility

Molecular Weight	272.09	Formula	C₅H₁₀N₂O₇P₂
CAS No.	118072-93-8	SDF	Download Zoledronic acid (Zoledronate) SDF
Smiles	C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

0.1M NAOH : 25 mg/mL (Ultrasonic and heating for 5 minutes.)

Water : 0.5 mg/mL (Warmed with 50℃ water bath; Ultrasonicated)

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

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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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.

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.

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