Deferasirox

Catalog No.S1712 Synonyms: CGP-72670, ICL-670

Deferasirox  Chemical Structure

Molecular Weight(MW): 373.36

Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 70 In stock
USD 120 In stock
USD 210 In stock
USD 470 In stock
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Cited by 2 Publications

1 Customer Review

  • U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox.

    Nature, 2014, 509(7498):105-9.. Deferasirox purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.
In vitro

Deferasirox effectively chelates iron from Rhizopus oryzae and demonstrates cidal activity in vitro against 28 of 29 clinical isolates of Mucorales at concentrations well below clinically achievable serum levels. [1] Deferasirox incubation induces a significant inhibition of NF-κB activity and a cytoplasmic sequestration of its active subunit p65 in an inactive form in 28 of 40 peripheral blood samples. [2] Deferasirox inhibits three human myeloid cell lines (K562, U937, and HL60) with IC50 of 17-50 mM. [3] Deferasirox is cidal in vitro against A. fumigatus, with an MIC and MFC of 25 and 50 mg/L, respectively. [5]

In vivo Deferasirox significantly improves survival and decreased tissue fungal burden in diabetic ketoacidotic or neutropenic mice with mucormycosis, with an efficacy similar to that of liposomal amphotericin B. Deferasirox treatment also enhances the host inflammatory response to mucormycosis. Deferasirox synergistically improves survival and reduces tissue fungal burden when combined with liposomal amphotericin B. [1] Deferasirox administered p.o. to rats is absorbed to at least 75%, and the bioavailability is 26%.Deferasirox is present in the blood circulation mainly in the unchanged form and as its iron complex, Fe(deferasirox)2, after intravenous and p.o. administration. Deferasirox is 99.2% bound to plasma proteins. [4] Deferasirox monotherapy modestly prolongs survival of mice with IPA. [5]

Protocol

Solubility (25°C)

In vitro DMSO 74 mg/mL (198.2 mM)
Ethanol 2 mg/mL (5.35 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* 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 373.36
Formula

C21H15N3O4

CAS No. 201530-41-8
Storage powder
in solvent
Synonyms CGP-72670, ICL-670

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03920657 Recruiting Drug: Deferasirox Myelodysplastic Syndromes Fondazione Italiana Sindromi Mielodisplastiche Onlus July 2019 Phase 2
NCT02663752 Terminated Procedure: Bone marrow aspirate|Drug: Deferasirox Myelodysplastic Syndrome Novartis Pharmaceuticals|Novartis May 30 2016 Phase 2
NCT02069886 Withdrawn Drug: deferasirox Thalassemia (Transfusion Delendent) Novartis Pharmaceuticals|Novartis December 2014 Phase 4
NCT02038816 Terminated Drug: Deferasirox + Azacitidine|Drug: Azacitidine Myelodysplastic Syndromes Sunnybrook Health Sciences Centre|Novartis March 2014 Phase 2

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.

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID