Deferasirox (Synonyms: ICL 670)

Name: Deferasirox
Brand: MedChemExpress
SKU: HY-17359
Rating: 5.0 (13 reviews)

Cat. No.: HY-17359 Purity: 99.86%: Data Sheet
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Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.

For research use only. We do not sell to patients.

CAS No. : 201530-41-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Deferasirox:

13 Publications Citing Use of MCE Deferasirox

Bio/Physico-chemical Assay

Microbiological Assay

Cell Imaging/Staining

: Deferasirox purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Mar 29;13(4):424.; Western blotting was conducted to assess the levels of autophagic markers (LC3B, ATG5, ATG12, and ATG16L1) in lysates of Sup-B15 and Molt-4 cells after Deferasirox (100 nM, 24 h) treatment.

: Deferasirox purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2024 Mar 29;13(4):424.; Intracellular ROS levels were measured as fold increases in fluorescence relative to the negative control after 0, 1, 2, 4, and 8 h exposures of Sup-B15 cells to Deferasirox (100 nM) treatment.

: Deferasirox purchased from MedChemExpress. Usage Cited in: Metallomics. 2024 Oct 4;16(10):mfae044. [Abstract]; Anaerobic Fe²⁺ competition binding assay for DFX, DFP, DMOG, and IOX3. Representative titration absorption spectra with corresponding binding profiles of Mag-Fura-2 competing for Fe²⁺ ions with Deferasirox.

: Deferasirox purchased from MedChemExpress. Usage Cited in: Bioengineered. 2022 Mar;13(3):6627-6637. [Abstract]; HK-2 cells were incubated in NG or HG conditions, and both were treated with DFX and erastin. Deferasirox (200 μM) treatment markedly suppressed LDH activity.

: Deferasirox purchased from MedChemExpress. Usage Cited in: Antioxidants. 2020 Aug 14;9(8):753. [Abstract]; Intensity of EPR spectra (arbitrary units) in the presence of PBN spin trapping agent in pRBCs treated with/without P505-15 (0.5 μΜ) for 24 h with/without 10-min incubation with DHA (200 µΜ) and with different concentrations (100–400 µM) of Deferasirox (DFX).

: Deferasirox purchased from MedChemExpress. Usage Cited in: Antioxidants. 2020 Aug 14;9(8):753. [Abstract]; Isobolograms showing the interactions between Syk Inhibitors (P505-15 and R406) and dihydroartemisinin (DHA) and artesunate (AS) in combination with the iron chelator Deferasirox (DFX), after 24 h of incubation in the P. falciparum Palo Alto strain. Synchronized P. falciparum cultures were treated for 24 h with different concentrations (from 0.05 to 2.5 µM) of representative Syk inhibitors (P505-15 and R406) in combination with different concentrations of DHA and AS (from 0.6 to 10 nM) using a fixed concentration (50 µM) of the iron chelator Deferasirox (DFX) at the ring stage.

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Biological Activity
Protocol
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Description

Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload^[1]^[2]^[3].

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	IC₅₀	3.4 μM Compound: 99	Antiproliferative activity against human DLD-1 cells assessed as reduction in cell proliferation Antiproliferative activity against human DLD-1 cells assessed as reduction in cell proliferation	[PMID: 33445154]
Fibroblast	IC₅₀	100 μM Compound: Deferasirox	Cytotoxicity against human foreskin fibroblasts after 96 hrs by MTT assay Cytotoxicity against human foreskin fibroblasts after 96 hrs by MTT assay	[PMID: 20005708]
HL-60	GI₅₀	5.5 μM Compound: 27a	Antiproliferative activity against human HL-60 cells Antiproliferative activity against human HL-60 cells	[PMID: 35838529]
MDA-MB-231	IC₅₀	4 μM Compound: Deferasirox	Cytotoxicity against human MDA-MB-231 cells after 96 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 96 hrs by MTT assay	[PMID: 20005708]
MIA PaCa-2	IC₅₀	10 μM Compound: Deferasirox	Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay	[PMID: 20005708]
NCI-H460	IC₅₀	20.36 μM Compound: DFX	Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 34292737]
NCI-H460	IC₅₀	98.35 μM Compound: DFX	Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 34292737]
SK-N-MC	IC₅₀	20.54 μM Compound: 3	Toxicity in human SK-N-MC cells by MTT method Toxicity in human SK-N-MC cells by MTT method	[PMID: 20041672]
SW480	IC₅₀	3.9 μM Compound: 99	Antiproliferative activity against human SW480 cells assessed as reduction in cell proliferation Antiproliferative activity against human SW480 cells assessed as reduction in cell proliferation	[PMID: 33445154]

In Vitro

In LX-2 cells treated with 50 μM deferasirox for 12 h, α1(I)procollagen expression is decreased by 25%, with maximal reductions (10-fold) seen following 24-120 h of treatment. Similarly, α-smooth muscle actin (αSMA) expression is significantly lower^[1]. Deferasirox had anti-proliferative effects on HL-60 or KG-1 myeloid leukemia cell lines at a concentration as low as 5 μM . The cytotoxicity is both dose and time dependent^[2]. The viability of both EL4 cells and L1210 cells incubated with deferasirox decrease in a concentration-dependent manner^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The tumor is significantly smaller in the SIO mice treated with deferasirox compared with control. Mice treated with DFX showed longer survival than the other groups. Deferasirox has a survival benefit for SIO leukemia murine model in terms of iron chelation and antileukemic therapy^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

373.36

Formula

C₂₁H₁₅N₃O₄

CAS No.

201530-41-8

Appearance

Solid

Color

White to light brown

SMILES

O=C(O)C1=CC=C(N2N=C(C3=CC=CC=C3O)N=C2C4=CC=CC=C4O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (267.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6784 mL	13.3919 mL	26.7838 mL
5 mM	0.5357 mL	2.6784 mL	5.3568 mL
10 mM	0.2678 mL	1.3392 mL	2.6784 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (261 KB) HNMR (134 KB) RP-HPLC (226 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Sobbe A, et al. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox. J Gastroenterol Hepatol. 2015 Mar;30(3):638-45. [Content Brief]

[2]. Kim JL, et al. The oral iron chelator deferasirox induces apoptosis in myeloid leukemia cells by targetingcaspase. Acta Haematol. 2011;126(4):241-5. [Content Brief]

[3]. Lee DH, et al. Deferasirox shows in vitro and in vivo antileukemic effects on murine leukemic cell lines regardless of iron status. Exp Hematol. 2013 Jun;41(6):539-46. [Content Brief]

Cell Assay ^[2]	Deferasirox is dissolved in DMSO. HL-60 or KG-1 cells are treated with 0, 5, 10, 50 μM of deferasirox for 24 or 48 h, and proliferation is determined by an MTT assay^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice: Murine leukemia cells are injected subcutaneously into the right flank of mice. Deferasirox is dissolved in distilled water and orally administered at 20 mg/kg until the cumulative dose reaches 300 mg/kg. The mice are observed and weighed daily^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Sobbe A, et al. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox. J Gastroenterol Hepatol. 2015 Mar;30(3):638-45. [Content Brief] [2]. Kim JL, et al. The oral iron chelator deferasirox induces apoptosis in myeloid leukemia cells by targetingcaspase. Acta Haematol. 2011;126(4):241-5. [Content Brief] [3]. Lee DH, et al. Deferasirox shows in vitro and in vivo antileukemic effects on murine leukemic cell lines regardless of iron status. Exp Hematol. 2013 Jun;41(6):539-46. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6784 mL	13.3919 mL	26.7838 mL	66.9595 mL
	5 mM	0.5357 mL	2.6784 mL	5.3568 mL	13.3919 mL
	10 mM	0.2678 mL	1.3392 mL	2.6784 mL	6.6960 mL
	15 mM	0.1786 mL	0.8928 mL	1.7856 mL	4.4640 mL
	20 mM	0.1339 mL	0.6696 mL	1.3392 mL	3.3480 mL
	25 mM	0.1071 mL	0.5357 mL	1.0714 mL	2.6784 mL
	30 mM	0.0893 mL	0.4464 mL	0.8928 mL	2.2320 mL
	40 mM	0.0670 mL	0.3348 mL	0.6696 mL	1.6740 mL
	50 mM	0.0536 mL	0.2678 mL	0.5357 mL	1.3392 mL
	60 mM	0.0446 mL	0.2232 mL	0.4464 mL	1.1160 mL
	80 mM	0.0335 mL	0.1674 mL	0.3348 mL	0.8370 mL
	100 mM	0.0268 mL	0.1339 mL	0.2678 mL	0.6696 mL

Deferasirox Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Deferasirox201530-41-8ICL 670ICL670ICL-670BacterialFerroptosisorallyavailableironchelatortransfusionaloverloadInhibitorinhibitorinhibit

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Deferasirox (Synonyms: ICL 670)

Customer Review

Other Forms of Deferasirox:

Deferasirox Related Antibodies

13 Publications Citing Use of MCE Deferasirox

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•Related Screening Libraries:

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Deferasirox Related Antibodies

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Complete Stock Solution Preparation Table

Deferasirox Related Classifications

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