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Busulfan Thioredoxin Reductase Inhibitor

Name: Busulfan
Brand: Selleck Chemicals
SKU: S1692
Availability: InStock
Rating: 5 (21 reviews)

Cat.No.S1692

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 (NSC-750) can be used to induce animal models of Anemia.

Chemical Structure

Molecular Weight: 246.3

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.81%

99.81

Related Targets	DNA/RNA Synthesis HDAC Topoisomerase PPAR PARP Sirtuin ATM/ATR Casein Kinase eIF MDM2/MDMX DNA-PK DHFR Nucleoside Analog/Antimetabolite DNA alkylator Telomerase Thymidylate Synthase CRISPR/Cas9 RAD51 BMI-1 LIM kinase RNR NUDIX High-mobility Group OGG1 MTH1 G-quadruplex SMN FENs WRN Pax

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	246.3	Formula	C₆H₁₄O₆S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	55-98-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC-750			Smiles	CS(=O)(=O)OCCCCOS(=O)(=O)C

Solubility

In vitro
Batch:

DMSO : 49 mg/mL (198.94 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.150mg/ml (12.79mM)	Taking the 1 mL working solution as an example, add 50 μL 63 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, 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.

Mechanism of Action

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. This compound inhibits the hematopoietic function of HSC alike cells and progenitors via an apoptosis-independent mechanism. It induces bone marrow hematopoietic cell senescence associated with an increased expression of p16^Ink4a and p19^Arf in a time-dependent manner. ^[1] This chemical, 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. It induces a transient reduction in GSH but a continuous increase in ROS production. ^[2] This compound-induced hypophosphorylation of Rb prevents apoptosis of spermatogonial stem cells by inhibiting PCNA expression in testicular cells. ^[3]
In vivo	Busulfan-treated mice exhibit a marked increase in apoptosis and a decrease in testis weight. This compound 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] Its conditioning and irradiation results in comparable sensitivity of HSC detection as evaluated by limiting dilution analysis in NOD/SCID mice. ^[4] This chemical-transplanted mice has slow and incomplete lymphoid engraftment. It (20 mg/kg to 100 mg/kg) provides dose-dependent congenic lymphoid reconstitution in mice. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/14500376/ [2] https://pubmed.ncbi.nlm.nih.gov/17512465/ [3] https://pubmed.ncbi.nlm.nih.gov/15388331/ [4] https://pubmed.ncbi.nlm.nih.gov/17018389/ [5] https://pubmed.ncbi.nlm.nih.gov/17018389/ [6] https://pubmed.ncbi.nlm.nih.gov/22286157/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-Y534 AR / AR Ack1 / Src		27904688
Growth inhibition assay	Cell viability		24815002

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
How can I reconstitute it 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 it in DMSO clearly first. Then add PEG and Tween. After they mixed well, dilute with water. It in this formulation is not suitable for long-term storage. Please make the fresh solution each time before use.

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