Name: Deferasirox (ICL670)
Brand: Selleck Chemicals
SKU: S1712
Availability: InStock
Rating: 5 (17 reviews)

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase DPP HIV Protease
Other P450 (e.g. CYP17) Inhibitors	Apigenin Baicalein Avasimibe Naringenin Diosmetin Alizarin Sodium Danshensu Naringin Benzbromarone Orteronel

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (200.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.700mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 74 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	373.36	Formula	C₂₁H₁₅N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	201530-41-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CGP-72670, ICL-670			Smiles	C1=CC=C(C(=C1)C2=NN(C(=N2)C3=CC=CC=C3O)C4=CC=C(C=C4)C(=O)O)O

Mechanism of Action

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. This compound 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. It inhibits three human myeloid cell lines (K562, U937, and HL60) with IC50 of 17-50 mM. The chemical is cidal in vitro against A. fumigatus, with an MIC and MFC of 25 and 50 mg/L, respectively.
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. This compound treatment also enhances the host inflammatory response to mucormycosis. It synergistically improves survival and reduces tissue fungal burden when combined with liposomal amphotericin B. This chemical administered p.o. to rats is absorbed to at least 75%, and the bioavailability is 26%. It 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. The compound is 99.2% bound to plasma proteins. It monotherapy modestly prolongs survival of mice with IPA.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17786247/ [2] https://pubmed.ncbi.nlm.nih.gov/20534700/ [3] https://pubmed.ncbi.nlm.nih.gov/19298223/ [4] https://pubmed.ncbi.nlm.nih.gov/18775980/ [5] https://pubmed.ncbi.nlm.nih.gov/19942619/

Applications

Methods	Biomarkers	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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Deferasirox (ICL670) CYP1A2 Inhibitor

Chemical Structure

Molecular Weight: 373.36