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Busulfan Thioredoxin Reductase Inhibitor

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

N. Cat.: S1692

Busulfan è un agente antineoplastico alchilante non specifico del ciclo cellulare. Causa DNA damage mediante la reticolazione di DNA, DNA e proteine. Busulfan inibisce l'attività della thioredoxin reductase. Induce anche apoptosis. È un agente chemioterapico immunosoppressivo e mieloablativo.Busulfan (NSC-750) può essere utilizzato per indurre modelli animali di Anemia.

Busulfan Alkylating Agent Chimico Chemical Structure

Struttura chimica

Peso molecolare: 246.3

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.81%

99.81

Target correlati	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Altro Alkylating Agent Inibitori	Berberine (Umbellatine) MNNG (1-Methyl-3-nitro-1-nitrosoguanidine)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	246.3	Formula	C₆H₁₄O₆S₂	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	55-98-1	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	NSC-750			Smiles	CS(=O)(=O)OCCCCOS(=O)(=O)C

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 49 mg/mL (198.94 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (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. 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. This compound-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. 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. Its conditioning and irradiation results in comparable sensitivity of HSC detection as evaluated by limiting dilution analysis in NOD/SCID mice. 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.
Riferimenti	[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/

Applicazioni (Applications)

Metodi	Biomarcatori	Immagini	PMID
Western blot	p-Y534 AR / AR Ack1 / Src		27904688
Growth inhibition assay	Cell viability		24815002

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2026-02-13)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT03538899	RECRUITING	Severe Combined Immunodeficiency	University of California, San Francisco	2018-05-31	PHASE1; PHASE2
NCT06851767	ENROLLING_BY_INVITATION	X-linked Severe Combined Immunodeficiency; X-SCID; XSCID	National Institute of Allergy and Infectious Diseases (NIAID)	2025-05-09	PHASE1; PHASE2
NCT07524530	NOT_YET_RECRUITING	Core Binding Factor Alpha Subunits; Hematologic Neoplasms; Leukemia; Lymphoma	National Cancer Institute (NCI)	2026-09-09	PHASE2
NCT05565105	NOT_YET_RECRUITING	Leukemia, Myeloid, Acute; Leukemia, Lymphocytic, Acute	Guenther Koehne	2026-06	PHASE2
NCT05617625	SUSPENDED	Myelodysplastic Syndromes; Graft Vs Host Disease; Graft-versus-host-disease	Guenther Koehne	2026-06	PHASE2
NCT01306019	RECRUITING	X-linked Severe Combined Immunodeficiency (XSCID)	National Institute of Allergy and Infectious Diseases (NIAID)	2012-09-25	PHASE1; PHASE2

Domande Frequenti (Frequently Asked Questions)

Domanda 1:
How can I reconstitute it for in vivo studies?

Risposta:
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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