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Busulfan

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Catalog No. T0923Cas No. 55-98-1
Alias Sulphabutin, Myleran, Busulphan

Busulfan is an alkylating antineoplastic agent derived from dimethane sulfonate, with cytotoxic and immunosuppressive properties. It primarily acts by forming carbonium ions in vivo, which induce cross-linking between DNA strands or between DNA and proteins, leading to DNA damage, inhibition of DNA replication, and suppression of RNA transcription. In addition, Busulfan can inhibit thioredoxin reductase and induce apoptosis. It is commonly used as a myeloablative agent in preconditioning regimens for bone marrow transplantation and can also be used to establish anemia models.

Busulfan

Busulfan

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Purity: 99.89%
Catalog No. T0923Alias Sulphabutin, Myleran, BusulphanCas No. 55-98-1
Busulfan is an alkylating antineoplastic agent derived from dimethane sulfonate, with cytotoxic and immunosuppressive properties. It primarily acts by forming carbonium ions in vivo, which induce cross-linking between DNA strands or between DNA and proteins, leading to DNA damage, inhibition of DNA replication, and suppression of RNA transcription. In addition, Busulfan can inhibit thioredoxin reductase and induce apoptosis. It is commonly used as a myeloablative agent in preconditioning regimens for bone marrow transplantation and can also be used to establish anemia models.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
500 mg$45In StockIn Stock
1 g$62In StockIn Stock
1 mL x 10 mM (in DMSO)$50In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.89%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Busulfan is an alkylating antineoplastic agent derived from dimethane sulfonate, with cytotoxic and immunosuppressive properties. It primarily acts by forming carbonium ions in vivo, which induce cross-linking between DNA strands or between DNA and proteins, leading to DNA damage, inhibition of DNA replication, and suppression of RNA transcription. In addition, Busulfan can inhibit thioredoxin reductase and induce apoptosis. It is commonly used as a myeloablative agent in preconditioning regimens for bone marrow transplantation and can also be used to establish anemia models.
In vitro
Mice transplanted with busulfan exhibit slow and incomplete lymphoid engraftment. Mice treated with busulfan demonstrate a significant increase in apoptosis and a reduction in testicular weight. In NOD/SCID mice, busulfan treatment combined with irradiation achieves a detection sensitivity similar to that of limiting dilution assays. A dose-dependent lymphoid tissue reconstitution is provided in mice with 20 mg/kg to 100 mg/kg of busulfan. At 40 mg/kg, busulfan induces the maximum number of apoptotic cells while minimizing the number of necrotic cells.
In vivo
Busulfan, an alkylating agent that induces DNA damage through cross-linking DNA with DNA and proteins, triggers senescence in normal human diploid WI38 fibroblast cells via a cascade mediated by extracellular signal-regulated kinase (Erk) and p38 mitogen-activated protein kinase (p38 MAPK), independent of the p53-DNA damage pathway. Busulfan causes a transient reduction in glutathione levels, followed by a sustained increase in ROS production. The hypophosphorylation of Rb induced by Busulfan inhibits the expression of PCNA in testicular cells, preventing apoptosis of spermatogonial stem cells. Moreover, while Busulfan reduces the frequency of cobblestone area-forming cells, it does not significantly increase apoptosis in hematopoietic stem cells (HSC)-like cells and progenitor cells with similar phenotypes. Busulfan suppresses the hematopoietic function of HSC-like cells and progenitor cells through an apoptosis-dependent mechanism. Additionally, Busulfan-induced senescence in bone marrow hematopoietic cells correlates with a time-dependent increase in the expression of p16Ink4a and p19Arf.
SynonymsSulphabutin, Myleran, Busulphan
Chemical Properties
Molecular Weight246.30
FormulaC6H14O6S2
Cas No.55-98-1
SmilesCS(=O)(=O)OCCCCOS(C)(=O)=O
Relative Density.1.35 g/cm3
Storage & Solubility Information
Storagestore under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50.00 mg/mL (203.00 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.00 mg/mL (12.18 mM)
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM4.0601 mL20.3004 mL40.6009 mL203.0045 mL
5 mM0.8120 mL4.0601 mL8.1202 mL40.6009 mL
10 mM0.4060 mL2.0300 mL4.0601 mL20.3004 mL
20 mM0.2030 mL1.0150 mL2.0300 mL10.1502 mL
50 mM0.0812 mL0.4060 mL0.8120 mL4.0601 mL
100 mM0.0406 mL0.2030 mL0.4060 mL2.0300 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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