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CAS No. 55-98-1
Busulfan (NSC-750) is a cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis.
Selleck's Busulfan (NSC-750) has been cited by 9 publications
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|Description||Busulfan (NSC-750) is a cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis.|
Busulfan inhibits the cobblestone area-forming cell frequency but fails to cause a significant increase in apoptosis in hematopoietic stem cell alike cells and progenitors. Busulfan inhibits the hematopoietic function of HSC alike cells and progenitors via an apoptosis-independent mechanism. Busulfan induces bone marrow hematopoietic cell senescence associated with an increased expression of p16Ink4a and p19Arf in a time-dependent manner.  Busulfan, an alkylating agent that causes DNA damage by cross-linking DNAs and DNA and proteins, induces senescence in normal human diploid WI38 fibroblasts through the extracellular signal-regulated kinase (Erk) and p38 mitogen-activated protein kinase (p38 MAPK) cascade independent of the p53-DNA damage pathway. Busulfan induces a transient reduction in GSH but a continuous increase in ROS production.  Busulfan-induced hypophosphorylation of Rb prevents apoptosis of spermatogonial stem cells by inhibiting PCNA expression in testicular cells. 
|In vivo||Busulfan-treated mice exhibit a marked increase in apoptosis and a decrease in testis weight. Busulfan is administered at the rate of 40 mg/kg body weight to induce a maximal number of apoptotic cells while minimizing the number of necrotic cells.  Busulfan conditioning and irradiation results in comparable sensitivity of HSC detection as evaluated by limiting dilution analysis in NOD/SCID mice.  Busulfan-transplanted mice has slow and incomplete lymphoid engraftment. Busulfan (20 mg/kg to 100 mg/kg) provides dose-dependent congenic lymphoid reconstitution in mice. |
-  Meng A, et al. Cancer Res, 2003, 63(17), 5414-5419.
-  Probin V, et al. Free Radic Biol Med, 2007, 42(12), 1858-1865.
-  Choi YJ, et al. FEBS Lett, 2004, 575(1-3), 41-51.
|In vitro||DMSO||49 mg/mL (198.94 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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 ddH2O，mix and clarify.
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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04451200||Not yet recruiting||Drug: Busulfan Injection||Acute Leukemia|Mielodysplasic Syndrome|Myeloproliferative Neoplasm||Institut Paoli-Calmettes||November 2020||Phase 2|
|NCT03601286||Recruiting||Drug: Lentiviral vector transduced CD34+ cells||Severe Combined Immunodeficiency X-Linked||Great Ormond Street Hospital for Children NHS Foundation Trust||December 21 2018||Phase 1|
|NCT03235973||Unknown status||Drug: Fludarabine-Cladribine-Busulfan conditioning regimen||Leukemia Myeloid Acute|Leukemia Lymphoblastic Acute||Institut Paoli-Calmettes||April 28 2018||Phase 1|
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Frequently Asked Questions
How can I reconstitute the drug for in vivo studies?
This compound also can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG and Tween. After they mixed well, dilute with water. S1692 in this formulation is not suitable for long-term storage. Please make the fresh solution each time before use.