| MDL | MFCD00058605 |
|---|---|
| Molecular Weight | 656.79 |
| Molecular Formula | C26H52N6O11S |
| SMILES | O=C(N(CCCCCN)O)CCC(NCCCCCN(C(CCC(NCCCCCN(C(C)=O)O)=O)=O)O)=O.CS(=O)(O)=O |
Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19 [1] [2] [3] [4] [5] .
Deferoxamine mesylate (1 mM; 16 h or 4 weeks) improves HIF-1α function under hypoxic and hyperglycemic conditions and decreases ROS in MEFs cells
[1]
.
Deferoxamine mesylate (100 µM; 24 h) increases InsR expression and activity and also induces an increase in p-Akt/total Akt/PKB levels
[2]
.
Deferoxamine mesylate (5, 10, 25, 50, 100 µM; 7 or 9 days) inhibits the proliferation of tumor-associated MSCs and bone marrow MSCs
[3]
.
Deferoxamine mesylate (5, 10, 25, 50, 100 µM; 7 days) induces apoptosis of MSCs
[3]
.
Deferoxamine mesylate (10 µM ; 3 days) influencs the expression of adhesion proteins on MSCs
[3]
.
Deferoxamine mesylate (100 µM; 24 h) induces autophagy mediated by the level of HIF-1α in SH-SY5Y cells
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | MEFs cells |
| Concentration: | 1 mM |
| Incubation Time: | 16 h (hypoxia condition); 4 weeks (hyperglycemic conditions) |
| Result: |
Significantly attenuated the hyperglycemia-associated increase in ROS levels under hypoxic high glucose conditions.
Notably increased normoxic HIF transactivation in MEFs under both high glucose and normal glucose conditions. |
Western Blot Analysis [2]
| Cell Line: | HepG2 cells |
| Concentration: | 100 µM |
| Incubation Time: | 24 h |
| Result: |
Showed a twofold increase of InsR mRNA levels in cells.
Increased by twofold InsR binding activity at the half-maximal concentration of 1.1 nM. |
Cell Proliferation Assay [3]
| Cell Line: | TAMSCs and BMMSCs (all isolated from Male C57BL/6J mice (8 week-old; EG-7 induced tumor model)) |
| Concentration: | 5, 10, 25, 50, 100 µM |
| Incubation Time: | 7 days (TAMSCs); 9 days (BMMSCs) |
| Result: | Inhibited the growth of TAMSCs and BMMSCs, and most cells are died at day 7 or 9 when exposed to 50 and 100 µM dose. |
Apoptosis Analysis [3]
| Cell Line: | TAMSCs, BMMSCs |
| Concentration: | 5, 10, 25, 50, 100 µM |
| Incubation Time: | 7 days |
| Result: | Exhibited proapoptotic effect on TAMSCs and BMMSCs cells. |
Western Blot Analysis [3]
| Cell Line: | TAMSCs, BMMSCs |
| Concentration: | 10 µM |
| Incubation Time: | 3 days |
| Result: | Remarkably decreased VCAM-1 expression in both TAMSCs and BMMSCs. |
Cell Autophagy Assay [4]
| Cell Line: | SH-SY5Y cells |
| Concentration: | 100 µM |
| Incubation Time: | 24 h |
| Result: |
Increased the ratio of LC3-II/I, an indicator of autophagy, which effects were blocked when autophagy-related gene
Beclin 1
was suppressed by
Beclin 1
siRNA transfection.
Caused a time and dose-dependent increase of HIF-1a, accompanied by the induction of autophagy. |
Deferoxamine mesylate (560.68 mg/per; drip-on; once daily for 21 days) enhances wound healing and increases neovascularization in aged or diabetic mice
[1]
.
Deferoxamine mesylate (200 mg/kg; i.p.; daily for 2 weeks) results in HIF-1α stabilization and increases glucose uptake, hepatic InsR expression, and signaling in vivo
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Aged (21-month-old) and diabetic (12-week-old) C57BL/6J mice (excisional wound model) [1] . |
| Dosage: | 560.68 mg/per (10 uL of 1 mM) |
| Administration: | Drip-on; once daily for 21 days. |
| Result: | Displayed significantly accelerated healing and increased neovascularization in both aged and diabetic mice model. |
| Animal Model: | Male Sprague-Dawley rats (180-200 g) [2] . |
| Dosage: | 200 mg/kg |
| Administration: | Intraperitoneal injection; daily for 2 weeks. |
| Result: | Significantly increased hepatic HIF-1α protein levels, InsR protein levels, as well as Akt/PKB and activated Akt/PKB were significantly higher in the liver. |
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00600938 | Novartis Pharmaceuticals|Novartis |
Transfusional Iron Overload|Transfusional Hemosiderosis
|
November 2007 | Phase 2 |
| NCT03137966 | Karolinska University Hospital |
Diabetic Foot Ulcer
|
December 30, 2022 | Phase 2 |
| NCT01254227 | Novartis Pharmaceuticals|Novartis |
Cardiac Iron Overload
|
January 2011 | Phase 2 |
| NCT04333550 | Kermanshah University of Medical Sciences |
COVID-19
|
April 2020 | Phase 1|Phase 2 |
| NCT00105495 | ApoPharma |
Thalassemia Major|Hemosiderosis
|
December 2002 | Phase 4 |
| NCT00115349 | HealthCore-NERI|National Heart, Lung, and Blood Institute (NHLBI) |
Cardiovascular Diseases|Heart Diseases|Beta-Thalassemia
|
June 2005 | Phase 2 |
| NCT04566991 | Aditya S. Pandey, MD|Michigan Medicine PKUHSC Joint Institute for Translational & Clinical Research|University of Michigan |
Aneurysmal Subarachnoid Hemorrhage
|
March 20, 2022 | Phase 2 |
| NCT04058197 | TauTona Group |
Chronic Cutaneous Ulcer|Sickle Cell Disease
|
July 21, 2020 | Phase 1|Phase 2 |
| NCT00000595 | National Heart, Lung, and Blood Institute (NHLBI) |
Anemia (Iron-Loading)|Beta-Thalassemia|Hematologic Diseases|Hemoglobinopathies|Thalassemia|Iron Overload|Hemochromatosis
|
January 1978 | Phase 2 |
| NCT04633889 | Brigham and Women´s Hospital|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
Acute Kidney Injury
|
April 13, 2021 | Phase 2 |
| NCT05300958 | Sun Yat-sen University |
Triple Negative Breast Cancer
|
March 21, 2022 | Phase 2 |
| NCT04361032 | Abderrahmane Mami Hospital|Eshmoun Clinical Research Center|Datametrix |
COVID19|Intensive Care Unit
|
September 4, 2020 | Phase 3 |
| NCT00598572 | Beth Israel Deaconess Medical Center|National Institute of Neurological Disorders and Stroke (NINDS)|Massachusetts General Hospital|Medical College of Wisconsin|Medical University of South Carolina|Hartford Hospital |
Intracerebral Hemorrhage
|
July 2008 | Phase 1 |
| NCT05184816 | Memorial Sloan Kettering Cancer Center|Center for Experimental Therapeutics|F.M. KIRBY FOUNDATION |
Leptomeningeal Metastases
|
December 22, 2021 | Phase 1 |
| NCT00870883 | Universidade do Extremo Sul Catarinense - Unidade Academica de Ciecias da Saude|Conselho Nacional de Desenvolvimento Científico e Tecnológico |
Hypotension|Acute Renal Failure
|
March 2009 | Phase 2 |
| NCT03652467 | Jinan Military General Hospital |
Hepatocellular Carcinoma Non-resectable
|
September 1, 2018 | Phase 1 |
| NCT02367248 | Capital Medical University|Beijing Tiantan Hospital|Peking University First Hospital|People´s Hospital of Beijing Daxing District|Beijing Haidian Hospital|The 263 Hospital of PLA|Beijing Aerospace General Hospital|Peking University Third Hospital|Beijing Pinggu District Hospital|Beijing Shuyi Hospital|General Hospital of Beijing PLA Military Region|Beijing Luhe Hospital|Beijing Fangshan District Liangxiang Hospital|Beijing Neurosurgical Institute|Beijing Jishuitan Hospital|Beijing Ditan Hospital|Beijing Youyi Hospital|Xiyuan Hospital of China Academy of Chinese Medical Sciences|Peking University People´s Hospital|The Second Artillery General Hospital|Chinese PLA General Hospital |
Intracerebral Hemorrhage
|
March 2015 | Phase 1|Phase 2 |
| NCT00777140 | Germans Trias i Pujol Hospital|Fundació Institut Germans Trias i Pujol |
Ischemic Stroke, Acute
|
September 2008 | Phase 2 |
| NCT00658411 | Dana-Farber Cancer Institute|Brigham and Women´s Hospital |
Acute Myeloid Leukemia|Acute Lymphoblastic Leukemia|Myelodysplastic Syndrome
|
August 2008 | Not Applicable |
| NCT00061750 | Novartis Pharmaceuticals|Novartis |
Beta-Thalassemia
|
May 2003 | Phase 3 |
| NCT00749515 | Boston Children´s Hospital|Novartis |
Transfusion-dependent Hemachromatosis|Thalassemia Major|Sickle Cell Disease
|
March 2008 | Phase 4 |
| NCT00000623 | HealthCore-NERI|National Heart, Lung, and Blood Institute (NHLBI)|Thalassemia Clinical Research Network |
Anemia, Cooley´s|Beta-Thalassemia|Hematologic Diseases|Thalassemia|Osteoporosis|Iron Overload|Hypertension, Pulmonary
|
July 2000 | |
| NCT04292314 | Beni-Suef University|Maternity and Children Hospital, Makkah|Beni-Suef Health insurance hospital|University of Arizona |
Iron Overload|Oxidative Stress|Thalassemia Major
|
November 1, 2019 | Phase 2|Phase 3 |
| NCT00738413 | Weill Medical College of Cornell University |
Thalassemia
|
August 2008 | Phase 1|Phase 2 |
| NCT00800761 | Ospedale Microcitemico|Azienda Sanitaria Locale di Cagliari |
Iron Overload|Cardiomyopathy
|
December 2001 | Phase 4 |
| NCT01459718 | Novartis Pharmaceuticals|Novartis |
Transfusion-dependent β-thalassemia Patients|Cardiac Iron Overload
|
January 2011 | Phase 2 |
| NCT02041299 | ApoPharma|Chiesi Canada Corp |
Iron Overload|Sickle Cell Disease|Other Anemias
|
April 17, 2014 | Phase 4 |
| NCT02175225 | Beth Israel Deaconess Medical Center|Medical University of South Carolina|National Institute of Neurological Disorders and Stroke (NINDS)|Massachusetts General Hospital|University of Massachusetts, Worcester|University of Pennsylvania|Johns Hopkins University|Duke University|University of North Carolina|University of Florida|Henry Ford Hospital|Ohio State University|St. Joseph´s Hospital and Medical Center, Phoenix|University of California, San Francisco|Oregon Health and Science University|Yale New Haven Health System Center for Healthcare Solutions|University of Iowa|Hartford Hospital|The University of Texas Health Science Center, Houston|Rhode Island Hospital|Stanford University|University of Washington|University of Calgary|Hopital de l´Enfant-Jesus|University of Alberta|Rush University Medical Center|University Hospitals Cleveland Medical Center|Columbia University|Weill Medical College of Cornell University|NYU Langone Health|Mount Sinai Hospital, New York|Loyola University |
Intracerebral Hemorrhage
|
October 2014 | Phase 2 |
| NCT00067080 | Novartis Pharmaceuticals|Novartis |
Anemia, Sickle Cell
|
May 2003 | Phase 2 |
| NCT01662895 | Beth Israel Deaconess Medical Center|Medical University of South Carolina|National Institute of Neurological Disorders and Stroke (NINDS)|Massachusetts General Hospital|Tufts Medical Center|University of Massachusetts, Worcester|University of Pennsylvania|Johns Hopkins University|University of Maryland|University of Virginia|Duke University|University of North Carolina|University of Florida|The Cleveland Clinic|Henry Ford Hospital|Ohio State University|St. Joseph´s Hospital and Medical Center, Phoenix|University of California, San Francisco|Oregon Health and Science University|Yale New Haven Hospital|University of Iowa|Hartford Hospital|The University of Texas Health Science Center, Houston|Rhode Island Hospital|Stanford University|University of Washington|University of Calgary|Hopital de l´Enfant-Jesus|University of Alberta|Dalhousie University |
Intracerebral Hemorrhage
|
March 18, 2013 | Phase 2 |
| NCT02875262 | Radboud University Medical Center|University Medical Center Groningen |
Intracranial Aneurysm|Subarachnoid Hemorrhage
|
December 1, 2017 | Phase 1|Phase 2 |
| NCT00110617 | Novartis Pharmaceuticals|Novartis |
Sickle Cell Disease|Iron Overload|Hemolytic Anemia
|
May 2005 | Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
H 2 O : 250 mg/mL ( 380.64 mM ; Need ultrasonic)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.5226 mL | 7.6128 mL | 15.2256 mL |
| 5 mM | 0.3045 mL | 1.5226 mL | 3.0451 mL |
| 10 mM | 0.1523 mL | 0.7613 mL | 1.5226 mL |
Add each solvent one by one: PBS
Solubility: 5.56 mg/mL (8.47 mM); Clear solution; Need ultrasonic