Clodronate Disodium

Catalog No.S4108

Clodronate Disodium Chemical Structure

Molecular Weight(MW): 288.86

Clodronate Disodium, a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.

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Biological Activity

Description Clodronate Disodium, a bisphosphonate, is a potent antiosteolytic agent which inhibits bone resorption.
In vitro

Clodronate significantly decreases total viability of cultures of J774 cells with EC50 of 300 μM, while liposome-encapsulated Clodronate decreases total viability of cultures of J774 cells with EC50 of 1 μM. Clodronate and liposome-encapsulated Clodronate is metabolized to a nonhydrolyzable adenosine triphosphate (ATP) analog, adenosine 5'-(beta, gamma-dichloromethylene) triphosphate, which can be detected in J774 cell extracts by using fast protein liquid chromatography. [1] Clodronate induces apoptosis in isolated osteoclasts. Clodronate, when administered in liposomes, also induces apoptosis in rat peritoneal macrophages in vitro and in liver macrophages of mice in vivo but not in murine macrophage-like RAW-264 cells. [2] Clodronate delivered into macrophages by liposome will kill these cells as a result of intracellular accumulation and irreversible metabolic damage. [3] Clodronate encapsulated in liposomes (clodrolip) efficiently depletes the phagocytic cells in the murine F9 teratocarcinoma and human A673 rhabdomyosarcoma mouse tumour models resulting in significant inhibition of tumour growth ranging from 75 to >92%, depending on therapy and schedule. [4] Clodronate, a bisphosphonate that lacks a nitrogen, does not inhibit protein isoprenylation but can be metabolized intracellularly to a beta-gamma-methylene (AppCp-type) analog of ATP, which is cytotoxic to macrophages in vitro. Clodronate is metabolited to AppCCl(2)p, and AppCCl(2)p inhibits mitochondrial oxygen consumption by a mechanism that involves competitive inhibition of the ADP/ATP translocase. [5]

Protocol

Solubility (25°C)

In vitro Water 72 mg/mL (249.25 mM)
DMSO Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 288.86
Formula

CH4Cl2O6P0.2Na

CAS No. 22560-50-5
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01348243 Completed Postmenopausal Osteoporosis Chiesi Farmaceutici S.p.A. October 2011 Phase 3
NCT01348243 Completed Postmenopausal Osteoporosis Chiesi Farmaceutici S.p.A. October 2011 Phase 3
NCT01291433 Completed Radiation Induced Brachial Plexopathy Assistance Publique - Hôpitaux de Paris March 2011 Phase 3
NCT01291433 Completed Radiation Induced Brachial Plexopathy Assistance Publique - Hôpitaux de Paris March 2011 Phase 3
NCT01198457 Completed Breast Neoplasms|Prostatic Neoplasms|Multiple Myeloma|Osteolysis Bayer January 2009 --
NCT01198457 Completed Breast Neoplasms|Prostatic Neoplasms|Multiple Myeloma|Osteolysis Bayer January 2009 --

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID