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Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.

For research use only. We do not sell to patients.

Cyclophosphamide Chemical Structure

Cyclophosphamide Chemical Structure

CAS No. : 50-18-0

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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Cyclophosphamide:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.

IC50 & Target

DNA Alkylator[1]

In Vitro

Cyclophosphamide induces outer membrane blebbing, leads to DNA fragmentation, as revealed by TUNEL staining of free 3'-OH DNA ends, and induces cleavage of the caspase 3 and caspase 7 substrate PARP in 9L/P450 cells. Bcl-2 expression fully blocks the activation of both initiator caspases as well as the effector caspase 3 in cells treated with activated Cyclophosphamide. Bcl-2 inhibits the cytotoxic effects but not the cytostatic effects of activated Cyclophosphamide[1]. Cyclophosphamide inhibits the AChE reversibly with an IC50 of 511 μM[2]. Carbon tetrachloride does not affect the direct cytotoxicity of cyclophosphamide or 4-hydroxycyclophosphamide to cells in culture[3].

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

In Vivo

Cyclophosphamide (CP) can be used to create models of premature ovarian failure, bone marrow suppression, and immunosuppression. It is enzymatically converted by liver enzymes (cytochrome P450) into the cytotoxic metabolite 4-hydroxycyclophosphamide (4OHCP). Cyclophosphamide exhibits significant interspecies and intraspecies kinetic variability. Dog microsomes catalyze the bioactivation of CP 55 times more efficiently than human microsomes, 2.8 times more efficiently than cat microsomes, and 1.2 times more efficiently than mouse microsomes.

Ovarian Failure Model[6]
Background
Cyclophosphamide (Cy) induces ovarian insufficiency (POI) via causes primordial follicle activation.
Specific Mmodeling Methods
Mice: Balb/C • female • 5-week-old
Administration: 150 mg/kg • ip • single dose.
Note
Modeling Indicators
Decreased number of primary follicles in the ovary.
Correlated Product(s): /
Opposite Product(s): HY-P74413

Myelosuppression and Immunosuppression[7]
Background
Cyclophosphamide induces myelosuppressi.on via interferes with the proliferation and differentiation of bone marrow (BM) cells.
Specific Mmodeling Methods
Mice: Swiss • male • 6-week-old
Administration: 150 mg/kg • ip • single dose.
Note
Modeling Indicators
Induced important changes in BM tissue structure, reduces the myeloid/erythroid ratio, and decreases the number of blood leukocytes.
Correlated Product(s): /
Opposite Product(s): HY-N0045

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

Animal Model: Six to eight-week old female C3H/HeN mice bearing SW1 tumors[4]
Dosage: 2 mg/mouse
Administration: Injected i.p.; 2mg/mouse in 0.1 mL PBS; 4 days
Result: Increased the percentage of cells that stained for CD3, CD4 or CD8 in both spleens and tumors.
Clinical Trial
Molecular Weight

261.09

Formula

C7H15Cl2N2O2P

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClCCN(CCCl)P1(OCCCN1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 38 mg/mL (145.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (127.66 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8301 mL 19.1506 mL 38.3011 mL
5 mM 0.7660 mL 3.8301 mL 7.6602 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.58 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 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 (9.58 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 25 mg/mL (95.75 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.8301 mL 19.1506 mL 38.3011 mL 95.7528 mL
5 mM 0.7660 mL 3.8301 mL 7.6602 mL 19.1506 mL
10 mM 0.3830 mL 1.9151 mL 3.8301 mL 9.5753 mL
15 mM 0.2553 mL 1.2767 mL 2.5534 mL 6.3835 mL
20 mM 0.1915 mL 0.9575 mL 1.9151 mL 4.7876 mL
25 mM 0.1532 mL 0.7660 mL 1.5320 mL 3.8301 mL
30 mM 0.1277 mL 0.6384 mL 1.2767 mL 3.1918 mL
40 mM 0.0958 mL 0.4788 mL 0.9575 mL 2.3938 mL
50 mM 0.0766 mL 0.3830 mL 0.7660 mL 1.9151 mL
60 mM 0.0638 mL 0.3192 mL 0.6384 mL 1.5959 mL
80 mM 0.0479 mL 0.2394 mL 0.4788 mL 1.1969 mL
100 mM 0.0383 mL 0.1915 mL 0.3830 mL 0.9575 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • 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.

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Cyclophosphamide
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