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Purity: ≥98%
Busulfan (Myleran; Busulfex IV) is a potent DNA alkylating agent with selective immunosuppressive effect on bone marrow. Since 1959, the approved cancer chemotherapy drug busulfan has been used in clinical settings. Within the alkyl sulfonate class of antineoplastics, busulfan is an alkylating agent that is non-specific to the cell cycle.
| ln Vitro |
Busulfan suppresses the frequency of cobblestone area-forming cells but does not significantly raise the rate of apoptosis in hematopoietic stem cell progenitors and similar cells. By an apoptosis-independent mechanism, busulfan inhibits the hematopoietic function of HSC progenitors and cells alike. In a time-dependent manner, busulfan causes bone marrow hematopoietic cell senescence, which is linked to an upregulation of p16Ink4a and p19Arf expression.[1] Normal human diploid WI38 fibroblasts are exposed to busulfan, an alkylating agent that damages DNA by cross-linking DNAs and DNA and proteins. This agent causes senescence through the extracellular signal-regulated kinase (Erk) and p38 mitogen-activated protein kinase (p38 MAPK) cascade, which is independent of the p53-DNA damage pathway. Busulfan causes a temporary decrease in GSH but a persistent rise in ROS generation.[2] By reducing the expression of PCNA in testicular cells, busulfan-induced hypophosphorylation of Rb stops spermatogonial stem cells from undergoing apoptosis.[3]
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| ln Vivo |
Busulfan-treated mice show a significant decrease in testis weight and an increase in apoptosis. In order to maximize the number of apoptotic cells and minimize the number of necrotic cells, 40 mg/kg body weight of busulfan is administered.[3] Using limiting dilution analysis, busulfan conditioning and radiation produce HSC detection sensitivity that is comparable in NOD/SCID mice.[4] Mice transplanted with busulfan exhibit incomplete and sluggish lymphoid engraftment. Mice that receive busulfan (20 mg/kg to 100 mg/kg) exhibit dose-dependent reconstitution of congenic lymphoid tissue.[5]
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| Cell Assay |
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. |
| Animal Protocol |
ICR male mice ranging in age from 8 to 12 weeks (30-40 g)
40 mg/kg (in sesame oil) IP; single dose |
| References |
| Molecular Formula |
C6H14O6S2
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|---|---|
| Molecular Weight |
246.3018
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| Exact Mass |
246.02
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| Elemental Analysis |
C, 29.26; H, 5.73; O, 38.98; S, 26.04
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| CAS # |
55-98-1
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| Related CAS # |
55-98-1 (Busulfan); 299-75-2 (Treosulfan); 52-24-4 (Thiotepa; Girostan; AI3-24916; NSC-6396)
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| Appearance |
Solid powder
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| SMILES |
CS(=O)(=O)OCCCCOS(=O)(=O)C
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| InChi Key |
COVZYZSDYWQREU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H14O6S2/c1-13(7,8)11-5-3-4-6-12-14(2,9)10/h3-6H2,1-2H3
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| Chemical Name |
4-methylsulfonyloxybutyl methanesulfonate
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| Synonyms |
Busulfex; Mitosan; Myleran; Mielucin; Misulban; Misulfan; BU; BUS; CB2041; GT41; WR19508
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| HS Tariff Code |
2905591000
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 63~125 mg/mL (255.8~507.5 mM)
Methanol: ~1 mg/mL (~4.1 mM) H2O: ~1 mg/mL (~4.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6.25 mg/mL (25.38 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (8.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: 5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 3.15mg/ml (12.79mM) Solubility in Formulation 6: 3.12 mg/mL (12.67 mM) in Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00534469 | Active Recruiting |
Drug: busulfan Drug: cytarabine |
Leukemia | City of Hope Medical Center | February 8, 2000 | Phase 2 |
| NCT00638898 | Active Recruiting |
Drug: busulfan Drug: melphalan |
Solid Tumor Ewing Sarcoma |
City of Hope Medical Center | February 26, 2007 | Phase 1 |
| NCT01798004 | Active Recruiting |
Drug: Busulfan Drug: Cisplatin |
Ganglioneuroblastoma Stage 1 Neuroblastoma |
Children's Oncology Group | April 8, 2013 | Phase 1 |
| NCT00534430 | Active Recruiting |
Drug: busulfan Drug: etoposide |
Myelodysplastic Syndromes Leukemia |
City of Hope Medical Center | February 29, 2000 | Phase 2 |
| NCT02250937 | Active Recruiting |
Drug: Busulfan Drug: Cladribine |
Acute Myeloid Leukemia Myelodysplastic Syndrome |
M.D. Anderson Cancer Center | October 27, 2014 | Phase 2 |
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