Biological Activity
Potent bisphophonate farnesyl diphosphate (FPP) synthase inhibitor (IC50 = 20 nM). Inhibits osteoclast-mediated bone resorption. Also inhibits Ras signaling and tumor growth, and induces apoptosis in pancreatic cancer cells. Reverses epithelial-mesenchymal transition and inhibits breast cancer cell renewal via inactivation of NF-κB.
Technical Data
| M. Wt | 272.09 |
| Formula | C5H10N2O7P2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 118072-93-8 |
| PubChem ID | 68740 |
| InChI Key | XRASPMIURGNCCH-UHFFFAOYSA-N |
| Smiles | OC(P(O)(O)=O)(P(O)(O)=O)CN1C=CN=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 0.68 | 2.5 | |
| 1.1eq. NaOH | 13.6 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 272.09. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.68 mL | 18.38 mL | 36.75 mL |
| 5 mM | 0.74 mL | 3.68 mL | 7.35 mL |
| 10 mM | 0.37 mL | 1.84 mL | 3.68 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.74 mL |
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References
References are publications that support the products' biological activity.
Schech et al (2013) Zoledronic acid reverses the epithelial-mesenchymal transition and inhibits self-renewal of breast cancer cells through inactivation of NF-κB. Mol.Cancer Ther. 12 1356 PMID: 23619300
Tassone et al (2003) Zoledronic acid induces antiproliferative and apoptotic effects in human pancreatic cancer cells in vitro. Br.J.Cancer 88 1971 PMID: 12799645
Dunford et al (2001) Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J.Pharmacol.Exp.Ther. 296 235 PMID: 11160603
Keywords: Zoledronic Acid, supplier, bisphosphonate, NF-KB, NF-kappaB, NF-κB, signaling, inhibitors, inhibits, potent, FPP, synthase, farnesyl, diphosphate, Ras, Zometa, Other, Synthases/Synthetases, NF-kB/IkB, G, Proteins, (Small), Cancer, Stem, Cells, Other, Synthases/Synthetases, Tocris Bioscience
