Home DNA Damage/DNA Repair DNA alkylator chemical - Apoptosis related activator Busulfan For research use only.

Busulfan

Synonyms: NSC-750

Busulfan is a cell cycle non-specific alkylating antineoplastic agent. It causes DNA damage by cross-linking DNAs and DNA and proteins. Busulfan inhibits thioredoxin reductase activity. It also induces apoptosis. It is an immunosuppressive and myeloablative chemotherapeutic agent.

Busulfan Chemical Structure

Busulfan Chemical Structure

CAS No. 55-98-1

Purity & Quality Control

Busulfan Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-SH cells Proliferation assay 10-100 μM 72 h Antiproliferative activity against human SK-N-SH cells at 10 to 100 uM after 72 hrs by MTT assay 24814532
SiMa cells Proliferation assay 10-100 μM 72 h Antiproliferative activity against human SiMa cells at 10 to 100 uM after 72 hrs by MTT assay 24814532
Kelly cells  Proliferation assay 10-100 μM 72 h Antiproliferative activity against human Kelly cells at 10 to 100 uM after 72 hrs by MTT assay 24814532
LS cells Proliferation assay 10-100 μM 72 h Antiproliferative activity against human LS cells at 10 to 100 uM after 72 hrs by MTT assay 24814532
K562 Apoptosis assay 48 hrs Induction of apoptosis in imatinib mesylate-resistant human K562 cells after 48 hrs 18339455
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
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Biological Activity

Description Busulfan is a cell cycle non-specific alkylating antineoplastic agent. It causes DNA damage by cross-linking DNAs and DNA and proteins. Busulfan inhibits thioredoxin reductase activity. It also induces apoptosis. It is an immunosuppressive and myeloablative chemotherapeutic agent.
In vitro
In vitro

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. [1] 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. [2] Busulfan-induced hypophosphorylation of Rb prevents apoptosis of spermatogonial stem cells by inhibiting PCNA expression in testicular cells. [3]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Y534 AR / AR Ack1 / Src 27904688
Growth inhibition assay Cell viability 24815002
In Vivo
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. [3] Busulfan conditioning and irradiation results in comparable sensitivity of HSC detection as evaluated by limiting dilution analysis in NOD/SCID mice. [4] 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. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04451200 Not yet recruiting
Acute Leukemia|Mielodysplasic Syndrome|Myeloproliferative Neoplasm
Institut Paoli-Calmettes
 November 2020 Phase 2
NCT03601286 Recruiting
Severe Combined Immunodeficiency X-Linked
Great Ormond Street Hospital for Children NHS Foundation Trust
 December 21 2018 Phase 1
NCT03235973 Unknown status
Leukemia Myeloid Acute|Leukemia Lymphoblastic Acute
Institut Paoli-Calmettes
 April 28 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 246.3 Formula

C6H14O6S2
CAS No. 55-98-1 SDF Download Busulfan SDF
Density 1.4 g/mL
Smiles CS(=O)(=O)OCCCCOS(=O)(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 49 mg/mL ( (198.94 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Frequently Asked Questions

Question 1:
How can I reconstitute the drug for in vivo studies?

Answer:
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.

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