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Zoledronic acid monohydrate Ras inhibitor

Name: Zoledronic acid monohydrate
Brand: Selleck Chemicals
SKU: S5244
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S5244

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.

Chemical Structure

Molecular Weight: 290.1

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Quality Control

Batch: S524401 0.5MNAOH]6.02 mg/mL]false]Water]2.3 mg/mL]false]DMSO]0.01 mg/mL]false Purity: 98%

Cited in Nature Medicine for its top-tier quality
COA
SDS/MSDS
Datasheet

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated KRas Aurora Kinase Casein Kinase
Other Ras Inhibitors	ERAS-0015 RMC-5127 Salirasib Kobe0065 RBC8 BQU57 CID-1067700 (ML282) ADT-007 NAV-2729 (Rac)-Antineoplaston A10

Solubility

In vitro
Batch:

0.5MNAOH : 6.02 mg/mL

Water : 2.3 mg/mL

DMSO : 0.01 mg/mL (0.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%0.5MNAOH 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.3mg/ml (1.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clarified 0.5MNAOH stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	290.1	Formula	C₅H₁₀N₂O₇P₂.H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	165800-06-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	zoledronate monohydrate, CGP-4244 monohydrate			SMILES	C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O.O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Ras Rho
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. 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 p21^ras. 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.
In vivo	Zoledronic acid affects breast cancer metastasis to visceral organs as well as bone. 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.]. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/14753746/ [2] https://pubmed.ncbi.nlm.nih.gov/12799645/ [3] https://pubmed.ncbi.nlm.nih.gov/15240548/ [4] https://pubmed.ncbi.nlm.nih.gov/12183663/ [5] https://pubmed.ncbi.nlm.nih.gov/19401351/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-04-20)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06374459	RECRUITING	Hormone Receptor Positive HER-2 Negative Metastatic Breast Cancer	Washington University School of Medicine	2025-01-30	PHASE1; PHASE2
NCT06767150	RECRUITING	Postmenopausal Osteoporosis	University Hospital, Toulouse	2025-10-02	PHASE4
NCT07406685	RECRUITING	Postmenopausal Osteoporosis; Postmenopausal Osteopenia; Primary Osteoporosis; Osteoporosis	National Taiwan University Hospital	2026-08-20	PHASE4
NCT06625190	RECRUITING	Neuroblastoma; Rhabdomyosarcoma; Synovial Sarcoma; Peripheral Nerve Sheath Tumors; Clear Cell Sarcoma; Alveolar Soft Part Sarcoma; Desmoplastic Small Round Cell Tumor; Chordoma; Rhabdoid Tumor; Epithelioid Sarcoma; Myoepithelial Tumor; Osteosarcoma; Ewing Sarcoma; Wilms Tumor	University of Florida	2026-02-11	PHASE1; PHASE2
NCT07772609	NOT_YET_RECRUITING	Osteoporosis in Post-menopausal Women	Sahlgrenska University Hospital	2027-01-11	PHASE4
NCT07668583	NOT_YET_RECRUITING	Osteomyelitis Chronic	Assistance Publique - Hôpitaux de Paris	2026-09-15	PHASE2

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