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Zoledronic Acid Potent nitrogen-containing bisphosphonates

Catalog No.A1352
Size Price Stock Qty
10mM (in 1mL DMSO)
$50.00
In stock
25mg
$50.00
In stock
100mg
$150.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Zoledronic Acid

Protocol

Cell experiment [1]:

Cell lines

The human breast carcinoma cell lines (MCF-7 and MDA-MB-231)

Preparation method

The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1–100 μM for 72 hours.

Applications

Treatment of MCF-7 cells with a range of zoledronic acid concentrations had little effect on apoptosis at 0.1 and 1.0 μM, however, an increase in the proportion of apoptotic cells was observed with 10 μM and 100 μM zoledronic acid compared with control (28.7% and 70.7% vs 22.57%, respectively).Treatment of MDA-MB-231 cells with 0.1–1 μM zoledronic acid did not cause an increase in apoptosis, but treatment with the 10 and 100 μM zoledronic acid resulted in a significant increase in the proportions of apoptotic cells (126.6% and 126.6% of control). A significant time-dependent increase in MCF7 cell apoptosis was confirmed when cells were incubated with 100 μM zoledronic acid for 24–96 hours.

Animal experiment [2]:

Animal models

The 5T2MM murine model (Male, 6-week-old, C57BL/KaLwRijHsd mice)

Dosage form

120 g/kg, subcutaneously (sc), twice weekly, 12 weeks.

Application

Treatment of mice bearing 5T2MM cells with zoledronic acid clearly prevented the development of osteolytic bone disease, decreased tumor burden in bone, and increased survival in a model of established myeloma.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Jagdev SP, Coleman RE, Shipman CM , et al .The bisphosphonate, zoledronic acid, induces apoptosis of breast cancer cells: evidence for synergy with paclitaxel. Br J Cancer. 2001 Apr 20;84(8):1126-34.

[2] Croucher PI, De Hendrik R, Perry MJ, et al. Zoledronic Acid Treatment of 5T2MM-Bearing Mice Inhibits the Development of Myeloma Bone Disease: Evidence for Decreased Osteolysis, Tumor Burden and Angiogenesis, and Increased Survival .J Bone Miner Res. 2003 Mar;18(3):482-92

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Chemical Properties

Cas No. 118072-93-8 SDF Download SDF
Chemical Name (1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid
Canonical SMILES C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O
Formula C5H10N2O7P2 M.Wt 272.09
Solubility Limited solubility Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Zoledronic acid, one of the most potent nitrogen-containing bisphosphonates, induces anti-proliferative and apoptotic effects on multiple myeloma cell lines in vitro by activating protein kinase C. Zoledronic acid also inhibits proliferation of human foet