Deferitrin
Based on 1 Customer Validation
Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major.
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- Pureté : 98.25%
- CAS No.: 239101-33-8
- Formule: C11H11NO4S
- Masse moléculaire:253.27
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| L1210 | IC50 |
19 μM
Compound: 8 ((S)-4'(HO)-DADFT)
|
Inhibitory concentration against growth of murine L1210 cells at 48 hours
Inhibitory concentration against growth of murine L1210 cells at 48 hours
|
[PMID: 15943485] |
| L1210 | IC50 |
20 μM
Compound: 8 ((S)-4'(HO)-DADFT)
|
Inhibitory concentration against growth of murine L1210 cells at 96 hours
Inhibitory concentration against growth of murine L1210 cells at 96 hours
|
[PMID: 15943485] |
In Vitro
The iron-clearing efficiency (ICE) of Deferitrin (GT-56-252) in a non-iron-overloaded rodent model after oral (po) administration at 300 μmol/kg is shown to be 1.1%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 239101-33-8
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Appearance Solid
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Masse moléculaire 253.27
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Formule C11H11NO4S
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Color Off-white to light yellow
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SMILES
O=C([C@]1(C)N=C(C2=CC=C(O)C=C2O)SC1)O
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Synonyms
GT-56-252
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (493.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Perls' Prussian Blue Iron Staining
Perls' Prussian blue staining is a histochemical method used to detect non-heme ferric iron (Fe3+) in biological tissues by exploiting an acid-mediated release of loosely bound iron from storage complexes such as ferritin or hemosiderin, followed by its reaction with potassium ferrocyanide to form an insoluble blue ferric ferrocyanide (Prussian blue) precipitate that marks iron localization under light microscopy. The reaction is classically performed under acidic conditions, which liberate Fe3+ ions that subsequently bind ferrocyanide to generate the visible chromogen, enabling spatial visualization of iron deposits in tissues such as brain, liver, and spleen. Histochemical interpretations are limited to a reactive iron pool rather than total iron content, reflecting only histologically accessible iron species rather than tightly protein-bound iron.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Raymond J Bergeron, et al. Design, Synthesis, and Testing of Non-Nephrotoxic Desazadesferrithiocin Polyether Analogues. J Med Chem. 2008 Jul 10;51(13):3913-23. [Content Brief]
[2]. Joanne M Donovan, et al. Preclinical and Clinical Development of Deferitrin, a Novel, Orally Available Iron Chelator. Ann N Y Acad Sci. 2005;1054:492-4. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9484 mL | 19.7418 mL | 39.4836 mL | 98.7089 mL |
| 5 mM | 0.7897 mL | 3.9484 mL | 7.8967 mL | 19.7418 mL | |
| 10 mM | 0.3948 mL | 1.9742 mL | 3.9484 mL | 9.8709 mL | |
| 15 mM | 0.2632 mL | 1.3161 mL | 2.6322 mL | 6.5806 mL | |
| 20 mM | 0.1974 mL | 0.9871 mL | 1.9742 mL | 4.9354 mL | |
| 25 mM | 0.1579 mL | 0.7897 mL | 1.5793 mL | 3.9484 mL | |
| 30 mM | 0.1316 mL | 0.6581 mL | 1.3161 mL | 3.2903 mL | |
| 40 mM | 0.0987 mL | 0.4935 mL | 0.9871 mL | 2.4677 mL | |
| 50 mM | 0.0790 mL | 0.3948 mL | 0.7897 mL | 1.9742 mL | |
| 60 mM | 0.0658 mL | 0.3290 mL | 0.6581 mL | 1.6451 mL | |
| 80 mM | 0.0494 mL | 0.2468 mL | 0.4935 mL | 1.2339 mL | |
| 100 mM | 0.0395 mL | 0.1974 mL | 0.3948 mL | 0.9871 mL |