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Busulfan Thioredoxin Reductase-remmer

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

Cat.Nr.: S1692

Busulfan is een celcyclus-niet-specifiek antineoplastisch Alkylating Agent. Het veroorzaakt DNA Damage/DNA Repair door het cross-linken van DNA's en DNA en eiwitten. Busulfan remt de Thioredoxin Reductase activiteit. Het induceert ook Apoptosis related. Het is een immunosuppressief en myeloablatief chemotherapeutisch middel.Busulfan (NSC-750) kan worden gebruikt om diermodellen van bloedarmoede te induceren.

Busulfan Alkylating Agent Chemisch Chemical Structure

Chemische structuur

Moleculair gewicht: 246.3

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.81%

99.81

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Overige Alkylating Agent Inhibitoren	Berberine (Umbellatine) MNNG (1-Methyl-3-nitro-1-nitrosoguanidine)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	246.3	Formule	C₆H₁₄O₆S₂	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	55-98-1	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NSC-750			Smiles	CS(=O)(=O)OCCCCOS(=O)(=O)C

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 49 mg/mL (198.94 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht 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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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 Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (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.
Referenties	[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/

Toepassingen (Applications)

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

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

Veelgestelde vragen (Frequently Asked Questions)

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

Antwoord:
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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