Art. -Nr.: HY-B0245

Busulfan

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

Busulfan is a potent alkylating antineoplastic agent. Busulfan causes DNA damage by cross-linking DNAs and DNA and proteins. Busulfan inhibits thioredoxin reductase. Busulfan induces apoptosis. Busulfan is an immunosuppressive and myeloablative chemotherapeutic agent.

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Reinheit: 99.90%
CAS. Nr.: 55-98-1
Formel: C₆H₁₄O₆S₂
Molecular Weight:246.30

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Busulfan Chemical Structure

CAS. Nr.: 55-98-1

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Induced Disease Models
- Clinical Trial
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	>100 μM Compound: Busulphan	In vitro cytotoxicity causing 50% growth inhibition was determined against A270 (human ovarian cancer)cell line In vitro cytotoxicity causing 50% growth inhibition was determined against A270 (human ovarian cancer)cell line	[PMID: 11277538]
Colon 26	IC₅₀	92.5 μM Compound: Busulphan	In vitro cytotoxicity causing 50% growth inhibition was determined against C26-10 (murine colon carcinoma) cell line In vitro cytotoxicity causing 50% growth inhibition was determined against C26-10 (murine colon carcinoma) cell line	[PMID: 11277538]
CWR22R	IC₅₀	24.3 μM Compound: Busulfan	Growth inhibition of human 22Rv1 cells after 5 days by SRB assay Growth inhibition of human 22Rv1 cells after 5 days by SRB assay	[PMID: 32484346]
DU-145	IC₅₀	25.8 μM Compound: Busulfan	Growth inhibition of human DU145 cells after 5 days by SRB assay Growth inhibition of human DU145 cells after 5 days by SRB assay	[PMID: 32484346]
H322	IC₅₀	>100 μM Compound: Busulphan	In vitro cytotoxicity causing 50% growth inhibition was determined against H322 (human non small cell lung cancer) cells In vitro cytotoxicity causing 50% growth inhibition was determined against H322 (human non small cell lung cancer) cells	[PMID: 11277538]
Lewis lung carcinoma cell line	IC₅₀	>100 μM Compound: Busulphan	In vitro cytotoxicity causing 50% growth inhibition was determined against LL (murine non small cell lung cancer) cell line In vitro cytotoxicity causing 50% growth inhibition was determined against LL (murine non small cell lung cancer) cell line	[PMID: 11277538]
PC-3	IC₅₀	36.2 μM Compound: Busulfan	Growth inhibition of human PC3 cells after 5 days by SRB assay Growth inhibition of human PC3 cells after 5 days by SRB assay	[PMID: 32484346]
UMSCC22B	IC₅₀	>100 μM Compound: Busulphan	In vitro cytotoxicity causing 50% growth inhibition was determined against 22B (human head and neck squamous) cell line In vitro cytotoxicity causing 50% growth inhibition was determined against 22B (human head and neck squamous) cell line	[PMID: 11277538]
WiDr	IC₅₀	>100 μM Compound: Busulphan	In vitro cytotoxicity causing 50% growth inhibition was determined against WiDr (human colon carcinoma) cell line In vitro cytotoxicity causing 50% growth inhibition was determined against WiDr (human colon carcinoma) cell line	[PMID: 11277538]

In Vitro

Busulfan (120 μM; 24 h) incited a moderate p53 activation, but strong Erk, p38, and JNK phosphorylation, in a time-dependent manner^[1].
Busulfan (120 μM; 24 h) results in premature senescence in WI38 cells via the Erk and p38 MAPK pathway, reduces GSH and increases ROS production, but the production can be suppressed by NADPH oxidase^[1].

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

Western Blot Analysis^[1]

Cell Line:

WI38 cells
Concentration:

120 μM
Incubation Time:

24 hours
Result:

Incited a moderate p53 activation, but strong Erk, p38, and JNK phosphorylation, in a time-dependent manner.
Elicited an immediate up-regulation of p21 expression, which subsided by day 11.

In Vivo

Animal Model:

ICR male mice ranging in age from 8 to 12 weeks (30-40 g) ^[4]
Dosage:

40 mg/kg (in sesame oil)
Administration:

IP; single dose
Result:

Increased apoptosis and decreased the testis weight in mice.
Exhibited higher level of pRB expression, inhibited Rb phosphorylation and PCNA expression compared to the control.

Induced Disease Models

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Busulfan can be used to induce aplastic anemia models. In mice, after injections of Busulfan at doses of 16.5 mg/kg and 33 mg/kg, the measured areas under the curve are 220±34 h·nmol·mL^-1 and 604±87 h·nmol·mL^-1, respectively^[7].

Induction of Aplastic Anemia Model^[6]

Background

Busulfan causes DNA damage by cross-linking DNA as well as DNA and proteins.

Specific Modeling Methods

Mice : ICR • male • 18-22 g, 6-8 weeks
Administration: 20 mg/kg busulfan+40 mg/kg cyclophosphamide• i.p. • one time per day for 12 days.

Note

(1) Twenty-four hours after the last intraperitoneal injection, tail vein blood was collected from eight mice randomly selected from each group for blood test.
(2) the mice are sacrificed by cervical dislocation and one femur was surgically dissected. After removing epiphysis from the femur, bone marrow cells are washed off using 1 ml PBS to prepare bone marrow cell suspension.

Modeling Indicators

The peripheral blood cells, hemoglobin, and bone marrow nucleated cells decreased significantly.
Histopathological: the proliferation of bone marrow hematopoietic tissues and cells was inhibited, and non-hematopoietic cells (fat cells) were significantly increased.

Correlated Product(s): Cyclophosphamide (HY-17420)

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 55-98-1
Appearance Solid
Molecular Weight 246.30
Formel C₆H₁₄O₆S₂
Color White to light brown
SMILES

CS(=O)(OCCCCOS(C)(=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (20)

All In Vivo Efficacy StudyFlow Cytometry

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Journal Impact Factor

J Extracell Vesicles

Extracellular Vesicles From Bone Marrow-Derived Macrophages Enriched in ARG1 Enhance Microglial Phagocytosis and Haematoma Clearance Following Intracerebral Haemorrhage. [Abstract]

2025 Jan;14(1):e70041. PMID: 39868438

Busulfan purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Jan;14(1):e70041. [Abstract]

20 mg/kg Busulfan was administered intraperitoneally every 2 days. Representative images of coronal brain sections from mice at 1, 3, and 7 days post-ICH showed residual haematomas. Scale bar, 5 mm.

Busulfan purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2025 Jan;14(1):e70041. [Abstract]

20 mg/kg Busulfan was administered intraperitoneally every 2 days. Quantification of residual haematoma index at 1, 3 and 7 days post-ICH and quantification of residual haemoglobin levels in the mouse brain.
Biomark Res

Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia. [Abstract]

2023 Jan 24;11(1):8. PMID: 36691065

Busulfan purchased from MedChemExpress. Usage Cited in: Biomark Res. 2023 Jan 24;11(1):8. [Abstract]

NSG mice were sub-lethally treated with Busulfan (30 mg/kg) 24 h before injection human AML cells harboring FLT3-ITD. The percentage of human CD45 positive cells in PB of PDX mice detected by flow cytometry on day 39 was recorded.
Cell Rep Med

A CD36-dependent non-canonical lipid metabolism program promotes immune escape and resistance to hypomethylating agent therapy in AML. [Abstract]

2024 Jun 18;5(6):101592. PMID: 38843841

Busulfan purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Jun 18;5(6):101592. [Abstract]

For primary PDXs, each NOG mouse was sublethally pretreated with Busulfan (30 mg/kg/day). NOG mice were intravenously implanted with BMMCs from patients with AML and were treated with or without fluvastatin for 2 weeks starting 7 days after implantation. Three days after the last treatment, percentages of human AML cells and human T cells in BM were tested.
J Neuroinflammation

Ly6C-high monocytes alleviate brain injury in experimental subarachnoid hemorrhage in mice. [Abstract]

2023 Nov 17;20(1):270. PMID: 37978532

Busulfan purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Nov 17;20(1):270. [Abstract]

Male mice were injected intraperitoneally with 140 μL of 6 mg/mL Busulfan for the ablation of bone marrow cells on days -7, -5, and -3 before BMT. The percentage of Ly6C-high monocytes on day 1 post-surgery was assessed by flow cytometry.
Stem Cell Res Ther

Clusterin-carrying extracellular vesicles derived from human umbilical cord mesenchymal stem cells restore the ovarian function of premature ovarian failure mice through activating the PI3K/AKT pathway. [Abstract]

2024 Sep 13;15(1):300. PMID: 39272156
Ecotoxicol Environ Saf

PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]

2025 Nov 15:307:119433. PMID: 41273832
Cells

Riluzole Reverses Blood-Testis Barrier Loss to Rescue Chemotherapy-Induced Male Infertility by Binding to TRPC. [Abstract]

2024 Dec 6;13(23):2016. PMID: 39682764
Toxicology

Exosomes-mediated retinoic acid disruption: A link between gut microbiota depletion and impaired spermatogenesis. [Abstract]

2024 Nov:508:153907. PMID: 39121937
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Water Biol Secur

2026 Mar 31.
J Radiat Res Appl Sci

2026 Mar 9.
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Reproduction

N-Carbamoylglutamate enhances bull spermatogenesis via Paraprevotella-mediated vitamin B6 biosynthesis in rumen microbiota. [Abstract]

2026 May 8;171(5):xaag049. PMID: 42081609
Mol Biol Cell

Mitotic DNA damage promotes chromokinesin-mediated missegregation of polar chromosomes in cancer cells. [Abstract]

2023 May 1;34(5):ar47. PMID: 36989031
Asian J Androl

Establishing a nonlethal and efficient mouse model of male gonadotoxicity by intraperitoneal busulfan injection. [Abstract]

2020 Mar-Apr;22(2):184-191. PMID: 31187778
Stem Cells Dev

Inhibiting Necroptosis of Spermatogonial Stem Cell as a Novel Strategy for Male Fertility Preservation. [Abstract]

2020 Apr 15;29(8):475-487. PMID: 32024413
Stem Cells Dev

Urine-Derived Stem Cells Facilitate Endogenous Spermatogenesis Restoration of Busulfan-Induced Nonobstructive Azoospermic Mice by Paracrine Exosomes. [Abstract]

2019 Oct 1;28(19):1322-1333. PMID: 31311428
Andrologia

Testicular quantitative ultrasound: A noninvasive monitoring method for evaluating spermatogenic function in busulfan-induced testicular injury mouse models. [Abstract]

2021 Mar;53(2):e13927. PMID: 33355959
Ann Transplant

Amniotic Fluid Transplantation Alleviates Hematopoietic Deficits in Experimental Rat Aplastic Anemia. [Abstract]

2021 Jan 8:26:e928047. PMID: 33414361
bioRxiv

Restoration of Spermatogenesis is Dependent on Activation of a SPRY4-ERK Checkpoint Following Germline Stem Cell Damage. [Abstract]

2025 Oct 14:2025.10.12.681919. PMID: 41279276

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (203.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Methanol : 1 mg/mL (4.06 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0601 mL

20.3004 mL

40.6009 mL

5 mM

0.8120 mL

4.0601 mL

8.1202 mL

10 mM

0.4060 mL

2.0300 mL

4.0601 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (8.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (8.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (8.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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: Corn Oil

Solubility: 3.12 mg/mL (12.67 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 6.25 mg/mL (25.38 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Probin V, et al. Busulfan-induced senescence is dependent on ROS production upstream of the MAPK pathway. Free Radic Biol Med. 2007 Jun 15;42(12):1858-65. Epub 2007 Mar 31. [Content Brief]

[2]. Mattan Levi, et al. Treosulfan induces distinctive gonadal toxicity compared with busulfan. Oncotarget. 2018 Apr 10;9(27):19317-19327. [Content Brief]

[3]. Janka Reimer, et al. Antineoplastic agent busulfan regulates a network of genes related to coagulation and fibrinolysis. Eur J Clin Pharmacol. 2012 Jun;68(6):923-35. [Content Brief]

[4]. Choi YJ, et al. Murine male germ cell apoptosis induced by busulfan treatment correlates with loss of c-kit-expression in a Fas/FasL- and p53-independent manner. FEBS Lett. 2004 Sep 24;575(1-3):41-51. [Content Brief]

[5]. Yoshida M, et al. Reduction of primordial follicles caused by maternal treatment with busulfan promotes endometrial adenocarcinoma development in donryu rats. J Reprod Dev. 2005 Dec;51(6):707-14. Epub 2005 Sep 22. [Content Brief]

[6]. Chen YF, et al. The role of RIP1 and RIP3 in the development of aplastic anemia induced by cyclophosphamide and busulphan in mice. Int J Clin Exp Pathol. 2014 Dec 1;7(12):8411-20. [Content Brief]

[7]. Bouligand J, et al. Induction of glutathione synthesis explains pharmacodynamics of high-dose busulfan in mice and highlights putative mechanisms of drug interaction. Drug Metab Dispos. 2007 Feb;35(2):306-14. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
Methanol / DMSO	1 mM	4.0601 mL	20.3004 mL	40.6009 mL	101.5022 mL
DMSO	5 mM	0.8120 mL	4.0601 mL	8.1202 mL	20.3004 mL
	10 mM	0.4060 mL	2.0300 mL	4.0601 mL	10.1502 mL
	15 mM	0.2707 mL	1.3534 mL	2.7067 mL	6.7668 mL
	20 mM	0.2030 mL	1.0150 mL	2.0300 mL	5.0751 mL
	25 mM	0.1624 mL	0.8120 mL	1.6240 mL	4.0601 mL
	30 mM	0.1353 mL	0.6767 mL	1.3534 mL	3.3834 mL
	40 mM	0.1015 mL	0.5075 mL	1.0150 mL	2.5376 mL
	50 mM	0.0812 mL	0.4060 mL	0.8120 mL	2.0300 mL
	60 mM	0.0677 mL	0.3383 mL	0.6767 mL	1.6917 mL
	80 mM	0.0508 mL	0.2538 mL	0.5075 mL	1.2688 mL
	100 mM	0.0406 mL	0.2030 mL	0.4060 mL	1.0150 mL

Keywords

Busulfan

20 Cited Publications

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Busulfan

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Publications Citing Use of MedChemExpress (MCE) Busulfan

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Busulfan Related Classifications

HY-B0245 Related Classifications