Deferiprone

Catalog No.S4067 Synonyms: CP20

For research use only.

Deferiprone (CP20) is a chelating agent with an affinity for ferric ion (iron III),binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable over a wide range of pH values.

Deferiprone Chemical Structure

CAS No. 30652-11-0

Selleck's Deferiprone has been cited by 9 Publications

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Biological Activity

Description Deferiprone (CP20) is a chelating agent with an affinity for ferric ion (iron III),binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable over a wide range of pH values.
Features Possesses 10-fold higher cytotoxicity than maltol in both HL-60 and HSC-2 cell lines.
In vitro

Deferiprone (100 μM) is able to protect myocytes from doxorubicin-induced lactate dehydrogenase release. Deferiprone (300 μM) quickly and efficiently removes iron(III) from its complex with doxorubicin. Deferiprone (300 μM) rapidly enters myocytes and displaces iron from a fluorescence-quenched trapped intracellular iron-calcein complex, suggesting that in the myocyte, deferiprone should also be able to displace iron from its complex with doxorubicin. Deferiprone (3 mM) also greatly reduces hydroxyl radical production by the iron(III)-doxorubicin complex in the xanthine oxidase/xanthine superoxide generating system. [1] Deferiprone (0.5 mM) increases removal of RBC membrane free iron in a time and dose dependent manner. [2] Deferiprone (0.3 mM) is effective in inhibiting radioactive iron mobilization from iron-loaded heart cells and protecting or restoring mitochondrial respiratory enzyme activity. Deferiprone (1 mM) results in a sharp decrease in complex I-III activity in iron-loaded heart cells. [3] Deferiprone shows cytotoxic effect of human tumor cell lines HSC-2, HSC-3 and HL-60 with IC50 of 13.5 μg/mL, 9.9 μg/mL and 10.6 μg/mL, the cytotoxic activity of HK1 against HL-60 and HSC-2 cells is reduced in the presence of FeCl3. Deferiprone (100 μg/mL) induces internucleosomal DNA fragmentation in HL-60 cells, but the addition of FeCl3 inhibits the DNA fragmentation. Deferiprone (100 μg/mL) activates the caspase 3, 8 and 9 in HSC-2 cells. [4]

In vivo Deferiprone (100 mg/kg) reduces the mean basilar artery cross-sectional areas by 24% in rabbits. Deferiprone (100 mg/kg) combined with subarachnoid hemorrhage(SAH) shows a variable amount of corrugation of the internal elastic lamina in rabbits. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 139.15
Formula

C7H9NO2

CAS No. 30652-11-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=O)C=CN1C)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02878538 Withdrawn Drug: Deferiprone|Other: Placebo phase Mild Cognitive Impairment The University of Texas Health Science Center at San Antonio January 2018 Early Phase 1
NCT02728843 Completed Drug: Deferiprone|Drug: Placebo Parkinson''s Disease ApoPharma October 12 2016 Phase 2
NCT02477631 Completed Drug: Deferiprone Myelodysplastic Syndrome With Low-grade Lesions|Iron Overload Due to Repeated Red Blood Cell Transfusions Sheba Medical Center|Hadassah Medical Organization|Tel Aviv Medical Center|Kaplan Medical Center|Ziv Medical Center February 2016 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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