Name: Tetraethylthiuram disulfide (Disulfiram)
Brand: Selleck Chemicals
SKU: S1680
Rating: 5 (48 reviews)

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Contrôle Qualité

Lot : Pureté : 99.91%

99.91

Cibles apparentées	HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Autre Dehydrogenase Inhibiteurs	Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Glycyrrhizin (Glycyrrhizic Acid, NSC 167409) Sodium Dichloroacetate (DCA) AGI-5198 Gossypol Acetate AGI-6780 Emodin NCT-503

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Temps dincubation	Description de lactivité	PMID
insect cells	Function assay	30 mins	Inhibition of recombinant human LOXL4 expressed in baculovirus infected insect cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.059 μM.	30098867
CHO	Function assay	30 mins	Inhibition of recombinant human LOXL3 expressed in CHO cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.093 μM.	30098867
MCF7	Antiproliferative assay	72 hrs	Antiproliferative activity against human MCF7 cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay, IC50 = 0.1 μM.	20222671
NS0	Function assay	30 mins	Inhibition of recombinant LOXL2 (unknown origin) expressed in NS0 cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.15 μM.	30098867
T47D	Antiproliferative assay	72 hrs	Antiproliferative activity against human T47D cells expressing BCA2 and estrogen receptor after 72 hrs by MTT assay, IC50 = 0.17 μM.	20222671
MDA-MB-231	Antiproliferative assay	72 hrs	Antiproliferative activity against human MDA-MB-231 cells expressing BCA2 and ERalpha after 72 hrs by MTT assay, IC50 = 0.32 μM.	20222671
HEK293	Function assay	30 mins	Inhibition of recombinant human LOX expressed in HEK293 cells using diaminopentane as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by fluorimetric method, IC50 = 0.32 μM.	30098867
CHO	Function assay		Agonist activity at human TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels, EC50 = 3 μM.	20356305
CEM-SS	Antiviral assay		Antiviral activity against HIV-1 in CEM-SS cells using XXT assay, IC50 = 3.9 μM.	9207937
MCF10A	Antiproliferative assay	72 hrs	Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay, IC50 = 10 μM.	20222671
HepG2	Cytotoxicity assay	72 hrs	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 38 μM.	29571571
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
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
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
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Informations chimiques, stockage et stabilité

Poids moléculaire	296.54	Formule	C₁₀H₂₀N₂S₄	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	97-77-8	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	NSC 190940, Tetraethylthiuram disulfide, TETD			Smiles	CCN(CC)C(=S)SSC(=S)N(CC)CC

Solubilité

In vitro
Lot:

DMSO : 59 mg/mL (198.96 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 59 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (16.86mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	3.900mg/ml (13.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 78 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	3.333mg/ml (11.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 66.67 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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.
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	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	4.000mg/ml (13.49mM)	Taking the 1 mL working solution as an example, add 100 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (16.86mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	2.500mg/ml (8.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	ALDH1 (Cell-free assay) 0.15 μM ALDH2 (Cell-free assay) 1.45 μM
In vitro	Le complexe Disulfiram-cuivre inhibe puissamment l'activité protéasomale dans les cellules de cancer du sein MDA-MB-231 et MCF10DCIS.com cultivées, mais pas les cellules normales et immortalisées MCF-10A, avant l'induction de la mort cellulaire apoptotique du cancer. Ce composé (DS), un médicament anti-alcoolisme cliniquement utilisé, inhibe fortement l'activité constitutive et induite par le 5-FU de NF-kappaB de manière dose-dépendante. Il inhibe la translocation nucléaire de NF-kappaB et l'activité de liaison à l'ADN, mais n'a aucun effet sur la dégradation d'IkappaBalpha induite par le 5-FU. Cette substance chimique améliore significativement l'effet apoptotique du 5-FU sur les lignées cellulaires DLD-1 et RKO(WT) et potentialise synergiquement la cytotoxicité du 5-FU pour les deux lignées cellulaires. Il abolit également efficacement la chimiorésistance au 5-FU dans une lignée cellulaire résistante au 5-FU H630(5-FU) in vitro. L'oseltamivir diminue le nombre de cellules viables, et l'ajout de CuCl(2) améliore significativement la mort cellulaire induite par le DSF à moins de 10% du contrôle. Ce composé, administré aux cellules de mélanome en combinaison avec Cu2+ ou Zn2+, diminue l'expression de la cycline A et réduit la prolifération in vitro à des concentrations plus faibles que le disulfiram seul.
In vivo	Disulfiram inhibe significativement la croissance tumorale (de 74 %), associée à une inhibition protéasomale in vivo (mesurée par la diminution des niveaux d'activité protéasomale du tissu tumoral et l'accumulation de protéines ubiquitinylées et de substrats naturels du protéasome p27 et Bax) et à l'induction de l'apoptose (comme le montrent l'activation de la caspase et la formation de noyaux apoptotiques) chez des souris porteuses de xénogreffes tumorales MDA-MB-231. Ce composé bloque la pompe d'extrusion de la P-glycoprotéine, inhibe le facteur de transcription nucléaire factor-kappaB, sensibilise les tumeurs à la chimiothérapie, réduit l'angiogenèse et inhibe la croissance tumorale chez les souris. Il inhibe la croissance et l'angiogenèse dans les mélanomes transplantés chez des souris immunodéficientes combinées sévères, et ces effets sont potentialisés par une supplémentation en Zn2+.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/17079463/ [2] https://pubmed.ncbi.nlm.nih.gov/12584750/ [3] https://pubmed.ncbi.nlm.nih.gov/15615540/ [4] https://pubmed.ncbi.nlm.nih.gov/15367699/ [5] https://pubmed.ncbi.nlm.nih.gov/9354647/ [6] https://pubmed.ncbi.nlm.nih.gov/32367036/

Informations sur lessai clinique

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT05626920	Recruiting	Inherited Retinal Dystrophy Primarily Involving Sensory Retina	University of Washington	December 2023	Phase 1\|Phase 2
NCT04485130	Terminated	Covid19	University of California San Francisco	August 18 2021	Phase 2
NCT03151772	Terminated	Glioblastoma	Sahlgrenska University Hospital Sweden	January 29 2018	Early Phase 1
NCT02309801	Completed	Healthy	Parc de Salut Mar\|Ministerio de Sanidad Servicios Sociales e Igualdad	July 2012	Phase 1

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Tetraethylthiuram disulfide (Disulfiram) inhibiteur de l'ALDH

Structure chimique

Poids moléculaire: 296.54