Cyclophosphamide

Name: Cyclophosphamide
Brand: MedChemExpress
SKU: HY-17420
Rating: 5.0 (27 reviews)

Cat. No.: HY-17420 Purity: ≥98.0%: FAQs
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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

CAS No. : 50-18-0

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100 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Cyclophosphamide:

27 Publications Citing Use of MCE Cyclophosphamide

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

DNA Alkylator^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
COS-1	IC₅₀	125.43 μM Compound: CYC-PHO	Cytotoxicity against african green monkey COS1 cells after 24 hrs by MTT assay Cytotoxicity against african green monkey COS1 cells after 24 hrs by MTT assay	[PMID: 23202484]
DU-145	IC₅₀	52.5 μM Compound: CPA	Cytotoxicity against human DU145 cells by MTT assay Cytotoxicity against human DU145 cells by MTT assay	[PMID: 21689869]
HCT-15	IC₅₀	74.32 μM Compound: CYC-PHO	Cytotoxicity against human HCT15 cells after 24 hrs by MTT assay Cytotoxicity against human HCT15 cells after 24 hrs by MTT assay	[PMID: 23202484]
HCT-15	IC₅₀	76.32 μM Compound: CYC-PHO	Growth inhibition of human HCT15 cells after 24 hrs by MTT assay Growth inhibition of human HCT15 cells after 24 hrs by MTT assay	[PMID: 28011220]
HEK-293T	IC₅₀	> 100 μM Compound: CYC-PHO	Growth inhibition of HEK293T cells after 24 hrs by MTT assay Growth inhibition of HEK293T cells after 24 hrs by MTT assay	[PMID: 28011220]
HEK-293T	IC₅₀	> 100 μM Compound: CP	Cytotoxicity against human HEK293T cells by MTT assay Cytotoxicity against human HEK293T cells by MTT assay	[PMID: 20850303]
HeLa	IC₅₀	71.4 μM Compound: CPA	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 21689869]
HEp-2	IC₅₀	> 100 μM Compound: CP	Cytotoxicity against human Hep2 cells by MTT assay Cytotoxicity against human Hep2 cells by MTT assay	[PMID: 20850303]
HepG2	IC₅₀	0.24 μM Compound: CP	Cytotoxicity against Homo sapiens (human) HepG2 cells after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) HepG2 cells after 48 hr by MTT assay	10.1007/s00044-011-9737-7
HepG2	IC₅₀	52.3 μM Compound: CYC-PHO	Growth inhibition of human HepG2 cells after 24 hrs by MTT assay Growth inhibition of human HepG2 cells after 24 hrs by MTT assay	[PMID: 28011220]
HepG2	IC₅₀	55.3 μM Compound: CYC-PHO	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 23202484]
HL-60	IC₅₀	8.79 μM Compound: CP	Cytotoxicity against human HL60 cells by MTT assay Cytotoxicity against human HL60 cells by MTT assay	[PMID: 20850303]
K562	IC₅₀	0.15 μM Compound: CP	Cytotoxicity against Homo sapiens (human) K562 cells after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) K562 cells after 48 hr by MTT assay	10.1007/s00044-011-9737-7
K562	IC₅₀	0.153 μM Compound: CP	Antiproliferative activity against Homo sapiens (human) K562 cells after 48 hr by MTT assay Antiproliferative activity against Homo sapiens (human) K562 cells after 48 hr by MTT assay	10.1007/s00044-010-9466-3
L1210	IC₅₀	> 300 μM Compound: Cyclophosphamide	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]
MCF7	IC₅₀	0.16 μM Compound: Cyclophosphamide	Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by trypan blue assay Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by trypan blue assay	10.1007/s00044-009-9222-8
MDA-MB-231	IC₅₀	0.09 μM Compound: CP	Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells after 48 hr by MTT assay	10.1007/s00044-011-9737-7
MDA-MB-231	IC₅₀	195.5 μM Compound: Cyclophosphamide	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	[PMID: 33139111]
NCI-H522	IC₅₀	67.9 μM Compound: CYC-PHO	Cytotoxicity against human NCI-H522 cells after 24 hrs by MTT assay Cytotoxicity against human NCI-H522 cells after 24 hrs by MTT assay	[PMID: 23202484]
NCI-H522	IC₅₀	69.9 μM Compound: CYC-PHO	Growth inhibition of human NCI-H522 cells after 24 hrs by MTT assay Growth inhibition of human NCI-H522 cells after 24 hrs by MTT assay	[PMID: 28011220]
PA-1	IC₅₀	64.12 μM Compound: CYC-PHO	Growth inhibition of human PA1 cells after 24 hrs by MTT assay Growth inhibition of human PA1 cells after 24 hrs by MTT assay	[PMID: 28011220]
PA-1	IC₅₀	64.12 μM Compound: CYC-PHO	Cytotoxicity against human PA1 cells after 24 hrs by MTT assay Cytotoxicity against human PA1 cells after 24 hrs by MTT assay	[PMID: 23202484]
T47D	IC₅₀	69 μM Compound: CYC-PHO	Growth inhibition of human T47D cells after 24 hrs by MTT assay Growth inhibition of human T47D cells after 24 hrs by MTT assay	[PMID: 28011220]
T47D	IC₅₀	70.1 μM Compound: CYC-PHO	Cytotoxicity against human T47D cells after 24 hrs by MTT assay Cytotoxicity against human T47D cells after 24 hrs by MTT assay	[PMID: 23202484]

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.

50-18-0

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 : 100 mg/mL (383.01 mM; Need ultrasonic; 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)

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
10 mM	0.3830 mL	1.9151 mL	3.8301 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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%

Select Batch:

Data Sheet (305 KB) SDS (584 KB)

COA (251 KB) HNMR (193 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Schwartz PS, et al. Cyclophosphamide induces caspase 9-dependent apoptosis in 9L tumor cells. Mol Pharmacol. 2001 Dec;60(6):1268-1279. [Content Brief]

[2]. al-Jafari AA, et al. Inhibition of human acetylcholinesterase by cyclophosphamide. Toxicology. 1995 Jan 19;96(1):1-6. [Content Brief]

[3]. Harris RN, et al. Carbon tetrachloride-induced increase in the antitumor activity of cyclophosphamide in mice: a pharmacokineticstudy. Cancer Chemother Pharmacol. 1984;12(3):167-72. [Content Brief]

[4]. Liu P, et al. Administration of cyclophosphamide changes the immune profile of tumor-bearing mice. J Immunother. 2010 Jan;33(1):53-9. [Content Brief]

[5]. Dominique A Ramirez, et al. Kinetics of Cyclophosphamide Metabolism in Humans, Dogs, Cats, and Mice and Relationship to Cytotoxic Activity and Pharmacokinetics. Drug Metab Dispos. 2019, 47, 3. [Content Brief]

[6]. H. Roness, et al. Pharmacological administration of recombinant human AMH rescues ovarian reserve and preserves fertility in a mouse model of chemotherapy, without interfering with anti-tumoural effects. J Assist Reprod Genet. 2019, 36, 9.

[7]. Susana Salva, et al. Probiotic Lactobacillus strains protect against myelosuppression and immunosuppression in cyclophosphamide-treated mice. Int Immunopharmacol. 2014, 22, 1. [Content Brief]

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.