Ferumoxytol
Based on 1 Customer Validation
Ferumoxytol is an FDA-approved ultrasmall superparamagnetic iron oxide preparation and iron replacement agent that exerts selective activity against leukemia cells with low ferroportin expression. Ferumoxytol increases intracellular iron levels, induces reactive oxygen species (ROS) production via the Fenton reaction, and triggers oxidative stress and cell death. Ferumoxytol reduces disease burden in mouse models and patient-derived leukemia models. As an MRI contrast agent, Ferumoxytol enables imaging of vascular lesions, tumors and lymph nodes. Ferumoxytol can be used in research related to acute myeloid leukemia and blast-phase chronic myeloid leukemia.
For research use only. We do not sell to patients.
- Purity: 95.00%
- CAS No.: 722492-56-0
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Storage:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
Ferumoxytol (24 h) significantly increases intracellular iron levels in human AML cell lines with low FPN expression, but exerts no such effect on human AML cell lines with high FPN expression[1].
Ferumoxytol (24-48 h) significantly reduces the viability of human acute myeloid leukemia (AML) cell lines and primary AML samples with low FPN expression, an effect mediated by oxidative stress, while human AML cell lines with high FPN expression are unaffected[1].
Ferumoxytol treatment upregulates the antioxidant stress response genes *SLC7A11*, *HMOX1* and *GCLC* in human AML cell lines with low FPN expression, and the extent of upregulation varies among different cell lines; in contrast, the expression of the aforementioned antioxidant genes shows no change in human AML cell lines with high FPN expression, and no upregulation of inflammatory cytokine genes is observed in any AML cell lines[1].
Ferumoxytol (24-48 h) significantly upregulates cytosolic and mitochondrial ROS levels in human acute myeloid leukemia (AML) cell lines with low FPN expression, and the increase in ROS levels correlates with decreased cell viability; in contrast, no significant change in ROS levels is observed in human AML cell lines with high FPN expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ferumoxytol (5 mg/kg; intravenous injection; twice weekly; for 4 consecutive weeks) selectively reduces the bone marrow engraftment rate of FPN-low-expressing AML PDX, without affecting FPN-high-expressing AML PDX or normal hematopoietic cells, and simultaneously induces oxidative stress in FPN-low-expressing leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6-8 weeks old, blast crisis chronic myeloid leukaemia induced by tail vein injection of 40 × 104 spleen cells carrying BCR-ABL/NUP98-HOXA9 oncogenes)[1]
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Dosage:3 mg/kg; 6 mg/kg
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Administration:i.v.; twice weekly; i.p.; three times weekly
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Result:Significantly reduced leukaemic blast percentage in peripheral blood, bone marrow, and spleen compared to saline controls.
Significantly lowered spleen index (spleen weight/body weight) compared to saline controls.
Significantly reduced peripheral blood leukaemic blast burden through day 21.
Increased median survival to 25 days compared to 17 days for saline controls.
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Animal Model:NOD/SCID; NSG (4-6 weeks old, acute myeloid leukaemia patient-derived xenografts established by tail vein injection of 2-5 million primary human AML cells with low ferroportin expression, following sub-lethal irradiation)[1]
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Dosage:5 mg/kg
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Administration:i.v.; twice weekly; 4 weeks
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Result:Significantly reduced human leukaemic cell engraftment percentage in bone marrow for three separate FPN-low AML PDX models (AML33, AML9, AML1) compared to saline controls.
Showed no reduction in FPN-high AML PDX or normal CD34+ cord blood xenografts.
Increased HMOX1 transcript levels in leukaemic cells from FPN-low AML PDXs by 2- to 6-fold, indicating increased oxidative stress.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 722492-56-0
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Appearance Liquid
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Color Light brown to brown
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SMILES
[Ferumoxytol]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Purity & Documentation
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Data Sheet (272 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Trujillo-Alonso V, et al. FDA-approved ferumoxytol displays anti-leukaemia efficacy against cells with low ferroportin levels. Nat Nanotechnol. 2019;14(6):616-622. [Content Brief]
[2]. Bashir MR, et al. Emerging applications for ferumoxytol as a contrast agent in MRI. J Magn Reson Imaging. 2015;41(4):884-898. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Ferumoxytol
- 722492-56-0
- Ferroptosis
- Reactive Oxygen Species (ROS)
- ferroportin-high leukaemia cells
- acute myeloid leukaemia
- FPN-low human AML cell lines
- reactive oxygen species
- normal haematopoietic cells
- Fenton reaction
- oxidative stress
- SLC7A11
- ferroportin-low leukaemia cells
- murine blast crisis chronic myeloid leukaemia models
- Inhibitor
- inhibitor
- inhibit