Zoledronic Acid

Description

Biological Activity

Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov)

Chemical Information

References

Name: Zoledronic Acid
Brand: Selleckchem
SKU: S1314

貨號 Cat. No.: S1314
規格 Size: 25mgã€00mg
品牌 Brand: Selleckchem

Zoledronic Acid

Catalog No.S13141 Product Citations

Zoledronic acid 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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25mg	USD 88	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 264	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01875458	Recruiting	Osteoporosis, With or Without Treatment\|Bisphosphonate Treatment\|Atypical Femur Fracture\|Bisphosphonate Related Osteonecrosis of the Jaws (BRONJ)\|Healthy Volunteers	University of Pennsylvania	2013-05
NCT01920568	Not yet recruiting	Fractures, Bone	GlaxoSmithKline\|Amgen	2013-08	Phase 3
NCT01702415	Withdrawn	Cystic Fibrosis	Papworth Hospital NHS Foundation Trust\|Novartis Pharmaceuticals	2013-10	Phase 4
NCT01951586	Recruiting	Non-Small Cell Lung Cancer	Amgen	2013-10	Phase 2
NCT01788176	Not yet recruiting	Complex Regional Pain Syndromes	University of Sao Paulo General Hospital\|Novartis	2013-12	Phase 2

Description

Zoledronic acid 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.

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]

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]

Download Zoledronic Acid SDF

Molecular Weight (MW)	272.09
Formula	C₅H₁₀N₂O₇P₂
CAS No.	118072-93-8

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	Zometa, Zomera, Aclasta and Reclast

Solubility (25°C) *	In vitro	DMSO	0.004 mg/mL (<1 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol,	10 mg/mL
* <1 mg/ml means slightly soluble or 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.