Home Proteases P450 (e.g. CYP17) chemical - Ferroptosis activator Deferasirox For research use only.

Deferasirox

Synonyms: CGP-72670, ICL-670

Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.

Deferasirox Chemical Structure

Deferasirox Chemical Structure

CAS No. 201530-41-8

Purity & Quality Control

Deferasirox Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 Cytotoxicity assay 96 hrs Cytotoxicity against human MDA-MB-231 cells after 96 hrs by MTT assay, IC50=4μM 20005708
MIAPaCa2 Cytotoxicity assay 96 hrs Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay, IC50=10μM 20005708
SK-N-MC Toxicity assay Toxicity in human SK-N-MC cells by MTT method, IC50=20.54μM 20041672
Sf9 Function assay 20 mins Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay, IC50=36.5μM 23956101
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.
In vitro
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot CDK2 / CDK4 / CDK6 / Cyclin A / Cyclin B / Cyclin D1 / Cyclin E / p53 / p27 / p21 TFR1 / Ferroportin Pro-caspase-3 / Pro-caspase-8 / Pro-caspase-9 / BAX / NDRG1 / c-Myc / p-mTOR 26965928
Immunofluorescence Bax / TOM22 Cytochrome c 28139717
Growth inhibition assay Cell viability Cell viability 26965928
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04423237 Recruiting
Iron Overload
University of Pisa|IRCCS Burlo Garofolo|University of Genova
 September 30 2020 --
NCT03920657 Terminated
Myelodysplastic Syndromes
Fondazione Italiana Sindromi Mielodisplastiche-ETS
 October 4 2019 Phase 2
NCT03372083 Completed
Iron Overload
Novartis Pharmaceuticals|Novartis
 January 16 2018 Phase 4
NCT02663752 Terminated
Myelodysplastic Syndrome
Novartis Pharmaceuticals|Novartis
 May 30 2016 Phase 2

Chemical Information & Solubility

Molecular Weight 373.36 Formula

C21H15N3O4
CAS No. 201530-41-8 SDF Download Deferasirox SDF
Smiles C1=CC=C(C(=C1)C2=NN(C(=N2)C3=CC=CC=C3O)C4=CC=C(C=C4)C(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (198.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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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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