4-Hydroperoxy cyclophosphamide [39800-16-3]

Référence HY-117433-5mg

Conditionnement : 5mg

Marque : MedChemExpress


Description

4-Hydroperoxy cyclophosphamide is the active metabolite form of the precursor Cyclophosphamide. 4-Hydroperoxy cyclophosphamide cross-links DNA to induce T cell apoptosis independent of caspase receptor activation, and can activate the mitochondrial death pathway by producing reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide can be used in the study of rheumatoid arthritis and autoimmune diseases[1][2].

Cellular Effect
Cell Line Type Value Description References
L1210 IC50
90 μM
Compound: 4-HC
Concentration required to reduce the viability of L1210 cells by 50% after 1-h incubation at 37 degrees C
Concentration required to reduce the viability of L1210 cells by 50% after 1-h incubation at 37 degrees C
[PMID: 1992116]
V79 IC50
2.7 μM
Compound: 4-hydroperoxycyclophosphamide
Antiproliferative activity against NTR expressing chinese hamster V79 cells after 72 hrs
Antiproliferative activity against NTR expressing chinese hamster V79 cells after 72 hrs
[PMID: 16821793]
V79 IC50
3.1 μM
Compound: 4-hydroperoxycyclophosphamide
Antiproliferative activity against chinese hamster V79 cells after 72 hrs
Antiproliferative activity against chinese hamster V79 cells after 72 hrs
[PMID: 16821793]
In Vitro

4-Hydroperoxy cyclophosphamide (1 or 3 μg/mL, 24, 48, 72 h) Apoptosis of Caspase-independent T cells is mediated by oxidative stress-induced mitochondrial apoptosis factor AIF and nuclear relocalization of EndoG[1].
4-Hydroperoxy cyclophosphamide (1 μg/mL, 72, 96 h) Combines with methotrexate (HY-14519), RANKL expression was inhibited in IL-6/ SIL-6R-induced fibroblast-like synoviocytes by inhibiting the JAK2/STAT3 and p38MAPK signaling pathways[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: CTL
Concentration: 3 μg/mL
Incubation Time: 24, 48, 72 h
Result: Increased the expression of p53 and Bax after 24 h.

Apoptosis Analysis[1]

Cell Line: Jurkat, CTL
Concentration: 1 or 3 μg/mL
Incubation Time: 24 , 48 , 72h
Result: Caspase-8 deficiency prevented CD95-mediated death induced by anti-CD95 monoclonal antibody (mAb) APO-1.
Overexpression of Bcl-2 inhibited apoptosis.
Induced cell death proceeded independently of caspase inhibition.
In Vivo

4-Hydroperoxy cyclophosphamide (200 mg/kg intraperitoneally injected) kills Caspase-independent T cells and B cells in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice[1]
Dosage: 200 mg/kg
Administration: i.p.
Result: Exhibited a marked depletion of immature double-positive CD4 þ CD8 þ thymocytes and mature single-positive CD4+ and CD8+ T cells.
Masse moléculaire

293.08

Formule

C7H15Cl2N2O4P

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=P1(OCCC(N1)OO)N(CCCl)CCCl

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvant et solubilité
In Vitro: 

DMSO : 50 mg/mL (170.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4120 mL 17.0602 mL 34.1204 mL
5 mM 0.6824 mL 3.4120 mL 6.8241 mL
View the 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (8.53 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (8.53 mM); 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.
Pureté et documentation
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