Deferasirox
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| Catalog No.GC11835 |
El deferasirox (ICL 670) es un quelante de hierro disponible por vÍa oral que se utiliza para el tratamiento de la sobrecarga transfusional de hierro.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 201530-41-8
Sample solution is provided at 25 µL, 10mM.
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Deferasirox is an orally active iron chelator used to treat iron overload diseases[1]. Deferasirox belongs to the family of N-substituted bishydroxyphenyltriazole tridentate iron chelators with antitumor activity[2]. Deferasirox is a potent nuclear factor-κB (NF-κB) inhibitor whose mechanism of action is independent of chelation-induced cellular iron deprivation[3].
In vitro, treatment of esophageal cancer OE33, OE19, and OE21 cells with Deferasirox (20μM) for 48h significantly increased transferrin receptor 1 (TfR1) mRNA and protein expression in the three cell lines, resulting in decreased cell viability and proliferation[4]. Treatment of LX-2 stellate cells with Deferasirox (50μM) for 12h significantly reduced the expression of α1(I) procollagen and α-smooth muscle actin (αSMA)[5].
In vivo, oral administration of Deferasirox (20mg/kg) to mice with secondary iron overload (SIO) inoculated with L1210 cells prolonged survival, reduced tumor volume, and decreased iron content in liver or tumor tissues[6]. Oral administration of Deferasirox (25mg/kg) to rats with iron poisoning significantly improved serum biochemical parameters[7].
References:
[1] Choudhry V P, Naithani R. Current status of iron overload and chelation with deferasirox[J]. The Indian Journal of Pediatrics, 2007, 74: 759-764.
[2] Barani M, Sargazi S, Hajinezhad M R, et al. Preparation of pH-responsive vesicular deferasirox: Evidence from in silico, in vitro, and in vivo evaluations[J]. ACS omega, 2021, 6(37): 24218-24232.
[3] Messa E, Carturan S, Maffè C, et al. Deferasirox is a powerful NF-κB inhibitor in myelodysplastic cells and in leukemia cell lines acting independently from cell iron deprivation by chelation and reactive oxygen species scavenging[J]. Haematologica, 2010, 95(8): 1308.
[4] Ford S J, Obeidy P, Lovejoy D B, et al. Deferasirox (ICL670A) effectively inhibits oesophageal cancer growth in vitro and in vivo[J]. British journal of pharmacology, 2013, 168(6): 1316-1328.
[5] Sobbe A, Bridle K R, Jaskowski L, et al. Inconsistent hepatic antifibrotic effects with the iron chelator deferasirox[J]. Journal of Gastroenterology and Hepatology, 2015, 30(3): 638-645.
[6] Lee D H, Jang P S, Chung N G, et al. Deferasirox shows in vitro and in vivo antileukemic effects on murine leukemic cell lines regardless of iron status[J]. Experimental Hematology, 2013, 41(6): 539-546.
[7] Rahdar A, Hajinezhad M R, Sargazi S, et al. Biochemical effects of deferasirox and deferasirox-loaded nanomicellesin iron-intoxicated rats[J]. Life Sciences, 2021, 270: 119146.
| Cell experiment [1]: | |
Cell lines | OE33, OE19, OE21 cells |
Preparation Method | All three oesophageal cell lines, OE33, OE19 and OE21, were incubated with Deferasirox (20μM) or Deferoxamine (10μM) for 48h/37°C. qRT-PCR was employed to assess levels of TfR1, ferritin-H and FPN mRNA relative to control cells. In addition, protein lysates were subject to Western blotting to assess protein levels of TfR1, ferritin-H and FPN. |
Reaction Conditions | 20μM; 48h |
Applications | Deferasirox treatment resulted in a significant increase in TfR1 mRNA and protein expression in all cell lines. Deferasirox treatment did not significantly alter ferritin-H mRNA and protein levels and FPN mRNA. |
| Animal experiment [2]: | |
Animal models | Non-SIO mice and secondary iron overload (SIO) mice bearing L1210 cells |
Preparation Method | Murine leukemia cells (L1210) were harvested, and 2×106 cells were injected subcutaneously into the right flank of mice anesthetized with 0.4% Avertin. After engraftment, the tumor size was measured three times per week with Vernier calipers. When tumor mass reaches visible size, the Deferoxamine group was given Deferoxamine (40mg/kg/day, i.p.) for 6 consecutive days, and the Deferasirox group was given Deferasirox (20mg/kg/day dissolved in 200mL distilled water, orally) until the cumulative dose reached 300mg/kg. The mice were observed and weighed daily. Liver and tumor tissues were collected immediately after death and preserved at -80℃ until iron content analysis was performed. The iron content of the liver and tumor tissues were measured using an atomic absorption spectrophotometer. |
Dosage form | 20mg/kg/day; p.o. |
Applications | The non-SIO mice and SIO mice bearing L1210 cells showed longer survival than other groups when treated with Deferasirox. The tumor was significantly smaller in the SIO mice treated with Deferasirox compared with the control group, the iron content of the liver or the tumor was decreased. |
References: | |
| Cas No. | 201530-41-8 | SDF | |
| Sinónimos | ICL 670 | ||
| Chemical Name | 4-[(3Z,5E)-3,5-bis(6-oxocyclohexa-2,4-dien-1-ylidene)-1,2,4-triazolidin-1-yl]benzoic acid | ||
| Canonical SMILES | C1=CC(=C2NC(=C3C=CC=CC3=O)N(N2)C4=CC=C(C=C4)C(=O)O)C(=O)C=C1 | ||
| Formula | C21H15N3O4 | M.Wt | 373.36 |
| Solubility | ≥100 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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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.
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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