Busulfan (Synonyms: Busulphan, Mielosan, Milecitan, Myeloleukon, Mylecytan, Myleran, NCI C01592, NSC 750) |
Katalog-Nr.GC13671
One-Click Copy Product Info
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Busulfan ist ein starker Alkylator mit selektiver immunsuppressiver Wirkung auf das Knochenmark.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 55-98-1
Sample solution is provided at 25 µL, 10mM.
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Busulfan is an alkylating drug alkylates DNA, with an IC50 value of 77μM for human serum Paraoxonase 1[1]. Busulfan has been widely used in cellular and animal models to induce rapidly dividing cell death[2].
In vitro, Busulfan treatment in P39 cells at 100μg/ml for 8 hours induced apoptosis, accompanied by caspase activation and cleavage of Bcl-2 and PARP proteins[3]. Treatment of HepaRG cells with 1000μM Busulfan for 4 days resulted in cellular mitochondrial dysfunction, elevated neutral lipid levels, increased fatty acid uptake, and decreased secretion of very-low-density lipoprotein[4]. Treatment of U2OS and MG-63 cells with 150μM Busulfan for 48 hours significantly inhibited cell viability, up-regulated the miR-200 family and regulated related target genes[5]. Treatment with 100μM Busulfan for 48 hours inhibited autophagy in mouse spermatogonial progenitor cells, resulting in a significant up-regulation of mTOR phosphorylation at Ser2448[6].
In vivo, Busulfan treatment via a single intraperitoneal injection at the dose of 40mg/kg for 56 days caused male C3H/Kam mice permanently infertile and led to the morphological damage to sperm produced by surviving stem cell spermatogonia[7]. In NOD/ LtSz-scid /IL2Rγ knockout mice, two intraperitoneal injections of 25mg/kg Busulfan at 48 and 24 hours before infusion of human cells promoted engraftment of human hematopoietic stem cell (HSC) and significantly improved survival[8].
References:
[1] Söyüt H. Investigation of inhibition of busulfan (Chemotherapeutic Drug) on human serum paraoxonase-1 (PON1)[J]. Int. J. Pharmacol. 2021, 17(8), 572–576.
[2] Berger D P, Winterhalter B R, Dengler W A, et al. Preclinical activity off hepsulfam and busulfan in solid human tumor xenografts and human bone marrow[J]. Anti-Cancer Drugs, 1992, 3(5): 531-540.
[3] Hassan Z, Hassan M, Hellström-Lindberg E. The pharmacodynamic effect of busulfan in the P39 myeloid cell line in vitro[J]. Leukemia, 2001, 15(8): 1240-1247.
[4] Allard J, Bucher S, Ferron P J, et al. Busulfan induces steatosis in HepaRG cells but not in primary human hepatocytes: Possible explanations and implication for the prediction of drug‐induced liver injury[J]. Fundamental & Clinical Pharmacology, 2024, 38(1): 152-167.
[5] Mei Q, Li F, Quan H, et al. Busulfan inhibits growth of human osteosarcoma through miR‐200 family micro RNA s in vitro and in vivo[J]. Cancer science, 2014, 105(7): 755-762.
[6] Wei R, Zhang X, Cai Y, et al. Busulfan suppresses autophagy in mouse spermatogonial progenitor cells via mTOR of AKT and p53 signaling pathways[J]. Stem Cell Reviews and Reports, 2020, 16(6): 1242-1255.
[7] Bucci L R, Meistrich M L. Effects of busulfan on murine spermatogenesis: cytotoxicity, sterility, sperm abnormalities, and dominant lethal mutations[J]. Mutation Research/Fundamental and Molecular Mechanisms of Mutagenesis, 1987, 176(2): 259-268.
[8] Hayakawa J, Hsieh M M, Uchida N, et al. Busulfan produces efficient human cell engraftment in NOD/LtSz-Scid IL2Rγ null mice[J]. Stem cells, 2009, 27(1): 175-182.
| Cell experiment [1]: | |
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Cell lines |
P39 cells |
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Preparation Method |
P39 cells were cultured in RPMI 1640 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS), penicillin (25IU/ml), and streptomycin (25μg/ml) at 37°C and 5% CO2 humidity. The cell seeding concentration was 0.20 × 106 cells /ml. All experiments were performed in exponentially growing cells. Cells were incubated with Busulfan at a final concentration of 10, 20, 40, 60, 80, and 100μg/ml for 2, 4, and 8 hours. The cells were washed and re-cultured for 72h in medium without Busulfan. In all experiments, cells cultured in medium supplemented with 10% FBS or medium supplemented with 10% FBS and 0.5% DMSO were used as controls. Cells treated with etoposide at a final concentration of 6μg/ml were used as a positive control for apoptosis. Cell number and viability were determined by the trypan blue exclusion assay. |
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Reaction Conditions |
10, 20, 40, 60, 80, and 100μg/ml; 2, 4, and 8h |
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Applications |
Busulfan inhibited cell viability and reduced cell number in a concentration and time-dependent manner within P39 cells. |
| Animal experiment [2]: | |
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Animal models |
Wistar rats |
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Preparation Method |
Thirty-two male Wistar rats (6-8 weeks old, with an average body weight of 150g) were housed under standard conditions (22 ± 3℃, humidity 45-60%), and had unlimited access to water and chewable food. The rats were randomly divided into 2 groups (8 rats in each group); (I): The control group of rats received no injections; (II): The rats in the second group were intraperitoneally injected with 40mg/kg Busulfan once. Samples were taken from the rats 56 days after the injection, and the histopathological changes were analyzed. |
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Dosage form |
40mg/kg for once; i.p. |
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Applications |
Busulfan treatment led to the depletion and destruction of sperm formation in rats, with congestion in the kidney tissue and extensive necrosis, degeneration and formation of hyaline casts in the renal tubules. |
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References: |
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| Cas No. | 55-98-1 | SDF | |
| Überlieferungen | Busulphan, Mielosan, Milecitan, Myeloleukon, Mylecytan, Myleran, NCI C01592, NSC 750 | ||
| Chemical Name | 4-methylsulfonyloxybutyl methanesulfonate | ||
| Canonical SMILES | CS(=O)(=O)OCCCCOS(=O)(=O)C | ||
| Formula | C6H14O6S2 | M.Wt | 246.3 |
| Löslichkeit | ≥ 12.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0601 mL | 20.3004 mL | 40.6009 mL |
| 5 mM | 812 μL | 4.0601 mL | 8.1202 mL |
| 10 mM | 406 μL | 2.03 mL | 4.0601 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)