Deferasirox
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MedKoo CAT#: 317140

CAS#: 201530-41-8

Description: Deferasirox is an oral iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long-term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It was approved by the United States Food and Drug Administration (FDA) in November 2005. Deferasirox seems to be capable of removing iron from cells (cardiac myocytes and hepatocytes) as well as removing iron from the blood.

Chemical Structure

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Deferasirox
CAS# 201530-41-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 317140
Name: Deferasirox
CAS#: 201530-41-8
Chemical Formula: C21H15N3O4
Exact Mass: 373.11
Molecular Weight: 373.370
Elemental Analysis: C, 67.56; H, 4.05; N, 11.25; O, 17.14

Price and Availability

Size Price Availability Quantity
100mg USD 150 Ready to ship
200mg USD 250 Ready to ship
500mg USD 450 Ready to ship
1g USD 650 Ready to ship
2g USD 950 Ready to ship
5g USD 1450 Ready to ship
10g USD 2450 Ready to ship
20g USD 3920 Ready to ship
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Synonym: ICL670; IC-L670; ICL 670; ICL-670A; ICL670A; IC L670A; Deferasirox. Brand name: Exjade; Desirox; Defrijet; Desifer.

IUPAC/Chemical Name: 4-(3,5-bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl)benzoic acid

InChi Key: BOFQWVMAQOTZIW-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H15N3O4/c25-17-7-3-1-5-15(17)19-22-20(16-6-2-4-8-18(16)26)24(23-19)14-11-9-13(10-12-14)21(27)28/h1-12,25-26H,(H,27,28)

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO (10mg/mL)

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.
In vitro activity: In LX-2 cells treated with 50 μM deferasirox for 12 h, α1(I)procollagen expression was decreased by 25%, with maximal reductions (10-fold) seen following 24-120 h of treatment. Similarly, α-smooth muscle actin (αSMA) expression was significantly lower. Alterations in matrix remodeling genes, specifically decreased expression of matrix metalloproteinase-2 and tissue inhibitor of metalloproteinase-2, were observed. Reference: J Gastroenterol Hepatol. 2015 Mar;30(3):638-45. https://doi.org/10.1111/jgh.12720
In vivo activity: To further study the in vivo antitumor activity of deferasirox (DFX) on tumor growth according to iron control, two mouse models were used (with or without SIO) bearing L1210 leukemic cells. In the first experiment, non-SIO mice were injected subcutaneously with L1210 cells. After 21 days of inoculation, non-SIO mice received PBS alone or ICAs according to the experimental design. The mice treated with DFX showed longer survival than the other groups (p = 0.017; Fig. 5). The initial size difference between tumors was large, preventing a meaningful statistical comparison of final tumor size (data not shown). The second experiment was performed with SIO mice. After 28 days of subcutaneous injection with L1210, the treatment for each mouse group was initiated. The SIO mice treated with DFX showed significantly longer survival than the SIO mice without treatment and the control mice (p < 0.01). The tumor size was significantly smaller in the SIO mice treated with DFX compared with the SIO mice without treatment and the control mice (p < 0.01). Reference: Exp Hematol. 2013 Jun;41(6):539-46. https://linkinghub.elsevier.com/retrieve/pii/S0301-472X(13)00017-9

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 74.0 198.20
Ethanol 15.0 40.18

Preparing Stock Solutions

The following data is based on the product molecular weight 373.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol: 1. Sobbe A, Bridle KR, Jaskowski L, de Guzman CE, Santrampurwala N, Clouston AD, Campbell CM, Subramaniam VN, Crawford DH. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox. J Gastroenterol Hepatol. 2015 Mar;30(3):638-45. doi: 10.1111/jgh.12720. PMID: 25168203.
In vivo protocol: 1. Lee DH, Jang PS, Chung NG, Cho B, Jeong DC, Kim HK. 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. doi: 10.1016/j.exphem.2013.02.004. Epub 2013 Feb 13. PMID: 23415674. 2. Sobbe A, Bridle KR, Jaskowski L, de Guzman CE, Santrampurwala N, Clouston AD, Campbell CM, Subramaniam VN, Crawford DH. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox. J Gastroenterol Hepatol. 2015 Mar;30(3):638-45. doi: 10.1111/jgh.12720. PMID: 25168203.

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1: Bruner KE, White KM. Deferasirox desensitization. J Allergy Clin Immunol Pract. 2015 Oct 15. pii: S2213-2198(15)00517-6. doi: 10.1016/j.jaip.2015.09.007. [Epub ahead of print] PubMed PMID: 26489716.

2: Ling G, Pinsk V, Golan-Tripto I, Ling E. Acute Liver Failure in a Pediatric Patient with Congenital Dysery-Thropoietic Anemia Type I Treated with Deferasirox. Hematol Rep. 2015 Sep 23;7(3):5987. doi: 10.4081/hr.2015.5987. eCollection 2015 Sep 23. PubMed PMID: 26487935.

3: Banerjee P, Sahoo A, Anand S, Bir A, Chakrabarti S. The Oral Iron Chelator, Deferasirox, Reverses the Age-Dependent Alterations in Iron and Amyloid-β Homeostasis in Rat Brain: Implications in the Therapy of Alzheimer's Disease. J Alzheimers Dis. 2015 Oct 17. [Epub ahead of print] PubMed PMID: 26484920.

4: Fragomeno C, Roccabruna E, D'Ascola DG. Effect of deferasirox on iron overload in patients with transfusion-dependent haemoglobinopathies. Blood Cells Mol Dis. 2015 Dec;55(4):382-6. doi: 10.1016/j.bcmd.2015.04.004. Epub 2015 Apr 22. PubMed PMID: 26460263.

5: Chang HH, Lu MY, Peng SS, Yang YL, Lin DT, Jou ST, Lin KH. The long-term efficacy and tolerability of oral deferasirox for patients with transfusion-dependent β-thalassemia in Taiwan. Ann Hematol. 2015 Dec;94(12):1945-52. doi: 10.1007/s00277-015-2476-y. Epub 2015 Sep 25. PubMed PMID: 26404899; PubMed Central PMCID: PMC4604499.

6: Marano M, Bottaro G, Goffredo B, Stoppa F, Pisani M, Marinaro AM, Deodato F, Dionisi-Vici C, Clementi E, Falvella FS. Deferasirox-induced serious adverse reaction in a pediatric patient: pharmacokinetic and pharmacogenetic analysis. Eur J Clin Pharmacol. 2015 Sep 24. [Epub ahead of print] PubMed PMID: 26403473.

7: Jaekel N, Lieder K, Albrecht S, Leismann O, Hubert K, Bug G, Kröger N, Platzbecker U, Stadler M, de Haas K, Altamura S, Muckenthaler MU, Niederwieser D, Al-Ali HK. Efficacy and safety of deferasirox in non-thalassemic patients with elevated ferritin levels after allogeneic hematopoietic stem cell transplantation. Bone Marrow Transplant. 2015 Sep 14. doi: 10.1038/bmt.2015.204. [Epub ahead of print] PubMed PMID: 26367238.

8: Nolte F, Angelucci E, Breccia M, Gattermann N, Santini V, Vey N, Hofmann WK. Updated recommendations on the management of gastrointestinal disturbances during iron chelation therapy with Deferasirox in transfusion dependent patients with myelodysplastic syndrome - Emphasis on optimized dosing schedules and new formulations. Leuk Res. 2015 Oct;39(10):1028-33. doi: 10.1016/j.leukres.2015.06.008. Epub 2015 Jun 20. Review. PubMed PMID: 26293555.

9: Latagliata R, Montagna C, Porrini R, Di Veroli A, Leonetti SC, Niscola P, Ciccone F, Spadea A, Breccia M, Maurillo L, Rago A, Spirito F, Cedrone M, De Muro M, Montanaro M, Andriani A, Bagnato A, Montefusco E, Alimena G. Chelation efficacy and erythroid response during deferasirox treatment in patients with myeloproliferative neoplasms in fibrotic phase. Eur J Haematol. 2015 Aug 16. doi: 10.1111/ejh.12674. [Epub ahead of print] PubMed PMID: 26277477.

10: Zeidan AM, Hendrick F, Friedmann E, Baer MR, Gore SD, Sasane M, Paley C, Davidoff AJ. Deferasirox therapy is associated with reduced mortality risk in a medicare population with myelodysplastic syndromes. J Comp Eff Res. 2015;4(4):327-40. doi: 10.2217/cer.15.20. PubMed PMID: 26274794.

11: Shaikh MS, Adil SN. Iron Chelation in Patients with Transfusion Dependent Thalassemia: An Insight on Response to Deferasirox. J Coll Physicians Surg Pak. 2015 Jul;25(7):553-4. doi: 07.2015/JCPSP.553554. PubMed PMID: 26208569.

12: Manduzio P. Deferasirox in a refractory anemia after other treatment options: case report and literature review. Clin Case Rep. 2015 Jun;3(6):361-7. doi: 10.1002/ccr3.262. Epub 2015 Mar 29. PubMed PMID: 26185629; PubMed Central PMCID: PMC4498843.

13: Vlachaki E, Agapidou A, Spanos G, Klonizakis P, Vetsiou E, Mavroudi M, Boura P. Five Years of Deferasirox Therapy for Cardiac Iron in β-Thalassemia Major. Hemoglobin. 2015 Oct;39(5):299-304. doi: 10.3109/03630269.2015.1064003. Epub 2015 Jul 15. PubMed PMID: 26177199.

14: Goswami D, Vitorino HA, Alta RY, Silvestre DM, Nomura CS, Machini MT, Espósito BP. Deferasirox-TAT(47-57) peptide conjugate as a water soluble, bifunctional iron chelator with potential use in neuromedicine. Biometals. 2015 Oct;28(5):869-77. doi: 10.1007/s10534-015-9873-5. Epub 2015 Jul 12. PubMed PMID: 26164834.

15: Ejaz MS, Baloch S, Arif F. Efficacy and adverse effects of oral chelating therapy (deferasirox) in multi-transfused Pakistani children with β-thalassemia major. Pak J Med Sci. 2015;31(3):621-5. doi: 10.12669/pjms.313.6972. PubMed PMID: 26150856; PubMed Central PMCID: PMC4485283.

16: Kohgo Y, Urabe A, Kilinç Y, Agaoglu L, Warzocha K, Miyamura K, Lim LC, Glaser S, Wang C, Wiktor-Jedrzejczak W. Deferasirox Decreases Liver Iron Concentration in Iron-Overloaded Patients with Myelodysplastic Syndromes, Aplastic Anemia and Other Rare Anemias. Acta Haematol. 2015 Jun 26;134(4):233-242. [Epub ahead of print] PubMed PMID: 26138856.

17: Karimi M, Arandi N, Haghpanah S, Ansari S, Azarkeyvan A, Bordbar M, Safaei S. Efficacy of Deferasirox (Exjade®) in Modulation of Iron Overload in Patients with β-Thalassemia Intermedia. Hemoglobin. 2015 Oct;39(5):327-9. doi: 10.3109/03630269.2015.1057735. Epub 2015 Jun 26. PubMed PMID: 26114738.

18: Lu MY, Wang N, Wu WH, Lai CW, Kuo PH, Chiang PH, Lin KH, Wu TH. Simultaneous Determination of Plasma Deferasirox and Deferasirox-Iron Complex Using an HPLC-UV System and Pharmacokinetics of Deferasirox in Patients With β-Thalassemia Major: Once-daily Versus Twice-daily Administration. Clin Ther. 2015 Aug 1;37(8):1751-60. doi: 10.1016/j.clinthera.2015.05.506. Epub 2015 Jun 18. PubMed PMID: 26093827.

19: Imanishi S, Takahashi R, Ohsuga M, Ohyashiki K, Ohyashiki JH. Effect of combined deferasirox and 5-azacytidine treatment on human leukemia cells in vitro. Ann Hematol. 2015 Sep;94(9):1601-2. doi: 10.1007/s00277-015-2417-9. Epub 2015 Jun 6. PubMed PMID: 26044890.

20: Chuang GT, Tsai IJ, Tsau YK, Lu MY. Transfusion-dependent thalassemic patients with renal Fanconi syndrome due to deferasirox use. Nephrology (Carlton). 2015 May 28. doi: 10.1111/nep.12523. [Epub ahead of print] PubMed PMID: 26016559.