2. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Ferroptosis Reactive Oxygen Species (ROS)
  4. Ferumoxytol

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.

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Ferumoxytol

Ferumoxytol Chemical Structure

CAS No. : 722492-56-0

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Ferumoxytol Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
In Vivo

Ferumoxytol (3-6 mg/kg; i.v., twice weekly; i.p., three times weekly) reduces leukemia blasts burden in the peripheral blood, bone marrow and spleen of mouse bcCML models, decreases the spleen index, and extends the median survival time by 8 days[1].
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.

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]
Dosage: 3 mg/kg; 6 mg/kg
Administration: i.v.; twice weekly; i.p.; three times weekly
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.
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]
Dosage: 5 mg/kg
Administration: i.v.; twice weekly; 4 weeks
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.
Clinical Trial
CAS No.
Appearance

Liquid

Color

Light brown to brown

SMILES

[Ferumoxytol]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL; Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
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Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 95.00%

SDS (418 KB)

COA (243 KB)

Handling Instructions (2659 KB)
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Ferumoxytol Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ferumoxytol722492-56-0FerroptosisReactive Oxygen Species (ROS)ferroportin-high leukaemia cellsacute myeloid leukaemiaFPN-low human AML cell linesreactive oxygen speciesnormal haematopoietic cellsFenton reactionoxidative stressSLC7A11ferroportin-low leukaemia cellsmurine blast crisis chronic myeloid leukaemia modelsInhibitorinhibitorinhibit

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