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5-Azacytidine (5-Aza, Azacitidine) DNA Methyltransferase Inhibiteur

Name: 5-Azacytidine (5-Aza, Azacitidine)
Brand: Selleck Chemicals
SKU: S1782
Rating: 5 (145 reviews)

Réf. CatalogueS1782

L'azacitidine (5-Azacytidine, 5-AzaC, Ladakamycine, AZA, 5-Aza, CC-486, NSC 102816) est un analogue nucléosidique de la cytidine qui inhibe spécifiquement la méthylation de l'ADN en piégeant les ADN méthyltransférases. L'azacitidine induit l'apoptose mitochondriale et l'autophagie.

5-Azacytidine (5-Aza, Azacitidine) DNA Methyltransferase Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 244.2

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.92%

99.92

Produits souvent utilisés avec 5-Azacytidine (5-Aza, Azacitidine)

Linifanib (ABT-869)

A cocktail consisting of this compound and Linifanib can turn fibroblasts into epithelial-like cells and activate OCT4.

UNC0379

It inhibits cell growth in PC9/ER and HCC827/ER cells, while UNC0379 has no significant effect on cell growth in these two cell lines.

Cibles apparentées	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Autre DNA Methyltransferase Inhibiteurs	RG108 (N-Phthalyl-L-Tryptophan) SGI-1027 Zebularine (NSC 309132) GSK3685032 Gamma-Oryzanol β-thujaplicin CM272 Bobcat339 DC-05 2'-Deoxy-5-Fluorocytidine

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Formulation	Description de l'activité	PMID
Raji	Growth Inhibition Assay	0.1-50 μM	12-72 h		inhibits cell growth in a dose dependent manner	26133246
Jurkat	Growth Inhibition Assay	0.1-50 μM	12-72 h		inhibits cell growth in a dose dependent manner	26133246
CA46	Function Assay	20 µM	48 h		increases PTPL1 mRNA expression	26133246
Raji	Function Assay	15 µM	48 h		increases PTPL1 mRNA expression	26133246
Jurkat	Function Assay	3.5 µM	48 h		increases PTPL1 mRNA expression	26133246
MDA-MB-231	Function Assay	1/2.5/5 μM	48 h		decreases the PTPN12 expression at the concerntration of 5 μM 48 h	25817229
MDA-MB-231	Function Assay	1/2.5/5 μM	48 h		increases the levels of E-cadherin mRNA at the concerntration of 2.5 μMfor 48 h	25817229
MDA-MB-231	Function Assay	1/2.5/5 μM	24/48 h		induces significant PARP cleavage after 48 h	25817229
MCF-7	Function Assay	1/2.5/5 μM	24/48 h		increases PARP cleavage	25817229
MDA-MB-231	Function Assay	1/2.5/5 μM	24/48 h		increases the expression of miRNA-124 at the concerntration of 5 μM	25817229
A498	Function Assay	10 µM	72 h		induces the ADAMTS18 gene expression	25569086
CaKI-2	Function Assay	10 µM	72 h		induces the ADAMTS18 gene expression	25569086
Ketr-3	Function Assay	10 µM	72 h		induces the ADAMTS18 gene expression	25569086
A253	Function Assay	10 µM	0-4 d		increases the mRNA expression level of the M3R after 24 h	25485536
A253	Function Assay	10 µM	72 h		increases the expression level of the M3R in both membrane and cytosolic preparations	25485536
A253	Function Assay	10 µM	0-4 d		reduces the 5-methylcytosine content	25485536
PC3	Function Assay	0.2 μM	4 d		increases the gene expression of IGFBP7, SFRP1 and SLC6A15 combined with GSK126	25477340
MCF7	Function Assay	0.3 μM	4 d		increases the gene expression of IGFBP7, SFRP1 and SLC6A15 combined with GSK126	25477340
PC3	Growth Inhibition Assay	0.2 μM	4 d		decreases the cell growth to 20.3% combined with GSK126	25477340
MCF7	Growth Inhibition Assay	0.3 μM	4 d		decreases the cell growth 24.8% combined with GSK126	25477340
BGC-823	Function Assay	5 μM	72 h		decreases the PRL-3 protein level signifcantly	25475733
MKN28	Function Assay	5 μM	72 h		decreases the PRL-3 protein level signifcantly	25475733
SGC-7901	Function Assay	5 μM	72 h		decreases the PRL-3 protein level signifcantly	25475733
MKN45	Function Assay	5 μM	72 h		decreases the PRL-3 protein level signifcantly	25475733
BGC-823	Function Assay	5 μM	72 h		decreases the mRNA expression of PRL-3 significantly	25475733
MKN28	Function Assay	5 μM	72 h		decreases the mRNA expression of PRL-3 significantly	25475733
SGC-7901	Function Assay	5 μM	72 h		decreases the mRNA expression of PRL-3 significantly	25475733
MKN45	Function Assay	5 μM	72 h		decreases the mRNA expression of PRL-3 significantly	25475733
HREC	Function Assay	5/10 μM	48 h		induces PEDF in a dose-dependent manner	25352747
HRPE	Function Assay	5/10 μM	48 h		induces PEDF in a dose-dependent manner	25352747
HREC	Function Assay	5/10 μM	48 h		down-regulates of VEGF, ICAM-1 (not protein level in HRPE cells), IL-1β dose-dependently	25352747
HRPE	Function Assay	5/10 μM	48 h		down-regulates of VEGF, IL-1β, and MMP2 dose-dependently	25352747
MSCs	Function Assay	10 μM	24 h		promotes the commitment of MSCs to myocardial differentiation	25351395
HL-60	Function Assay	5 μM	72 h	DMSO	significantly upregulates ZNF382 expression	25319049
MV4-11	Function Assay	5 μM	72 h	DMSO	significantly upregulates ZNF382 expression	25319049
A2780	Function Assay	5 µM	7 d		increases DNA methylation level	25299694
CP70	Function Assay	5 µM	7 d		increases DNA methylation level	25299694
A2780	Function Assay	5 µM	7 d		weakens the level of methylation	25299694
CP70	Function Assay	5 µM	7 d		weakens the level of methylation	25299694
OCM3	Growth Inhibition Assay	0.5/1/2 μM	7 d	DMSO	inhibits cell growth in a dose dependent manner	25146981
92.1	Growth Inhibition Assay	0.5/1/2 μM	7 d	DMSO	inhibits cell growth in a dose dependent manner	25146981
OCM1	Growth Inhibition Assay	0.5/1/2 μM	7 d	DMSO	inhibits cell growth in a dose dependent manner	25146981
OMM1	Growth Inhibition Assay	0.5/1/2 μM	7 d	DMSO	inhibits cell growth in a dose dependent manner	25146981
Mel 285	Growth Inhibition Assay	0.5/1/2 μM	7 d	DMSO	inhibits cell growth in a dose dependent manner	25146981
Mel 290	Growth Inhibition Assay	0.5/1/2 μM	7 d	DMSO	inhibits cell growth in a dose dependent manner	25146981
OCM3	Function Assay	0.5/1 μM	48 h	DMSO	decreases clonogenicity dose-dependently	25146981
92.1	Function Assay	0.5/1 μM	48 h	DMSO	decreases clonogenicity dose-dependently	25146981
OCM1	Function Assay	0.5/1 μM	48 h	DMSO	decreases clonogenicity dose-dependently	25146981
OMM1	Function Assay	0.5/1 μM	48 h	DMSO	decreases clonogenicity dose-dependently	25146981
Mel 285	Function Assay	0.5/1 μM	48 h	DMSO	decreases clonogenicity dose-dependently	25146981
Mel 290	Function Assay	0.5/1 μM	48 h	DMSO	decreases clonogenicity dose-dependently	25146981
OCM3	Function Assay	0.5/1 μM	48 h	DMSO	decreases invasion dose dependently	25146981
Mel 290	Function Assay	0.5/1 μM	48 h	DMSO	decreases invasion dose dependently	25146981
OMM1	Function Assay	0.5/1 μM	48 h	DMSO	decreases invasion dose dependently	25146981
OCM1	Cell Viability Assay	0.5/1 μM	5 d	DMSO	decreases radiation-induced cell viability inhibition	25146981
92.1	Cell Viability Assay	0.5/1 μM	5 d	DMSO	decreases radiation-induced cell viability inhibition	25146981
OCM1	Function Assay	0.5/1 μM	48 h	DMSO	causes global DNA hypomethylation at L-1 repeat loci	25146981
OCM3	Function Assay	0.5/1 μM	48 h	DMSO	causes global DNA hypomethylation at L-1 repeat loci	25146981
92.1	Function Assay	0.5/1 μM	48 h	DMSO	causes global DNA hypomethylation at L-1 repeat loci	25146981
IMR32	Function Assay	3 μM	72 h	DMSO	induces p19-INK4d expression significantly	25104850
IMR5-75	Function Assay	3 μM	72 h	DMSO	induces p19-INK4d expression significantly	25104850
Be(2)-C	Function Assay	3 μM	72 h	DMSO	induces p19-INK4d expression significantly	25104850
Bxpc-3	Growth Inhibition Assay	5/10 μM	24/48/72 h		inhibits the proliferation of Bxpc-3 cells in time- and concentration-dependent manners	25061731
Bxpc-3	Apoptosis Assay	5/10 μM	24/48/72 h		induces apoptosis in time- and concerntration manners	25061731
Bxpc-3	Function Assay	5/10 μM	24/48/72 h		decreases β-catenin expression after 24 h	25061731
Bxpc-3	Function Assay	5/10 μM	24/48/72 h		decreases cyclinD1 expression at the concerntration of 10 μM	25061731
Bxpc-3	Function Assay	5/10 μM	24/48/72 h		down-regulateS c-myc mRNA expression in time- and concentration-dependent manners	25061731
HL-60	Growth Inhibition Assay	1.0 μM	48 h		significantly inhibits HL-60 cell growth	25051119
HL-60	Function Assay	1.0 μM	48 h		increases p21WAF1/CIP1 and caspase-3 expression	25051119
HL-60	Function Assay	1.0 μM	48 h		decreases Bcl-xL expression significantly	25051119
HuTu-80	Function Assay	1/5/10 μM	48/72 h		increases the expression of human NPC1L1 mRNA in a dose-dependent manner	24904062
Caco2	Function Assay	10 μM	48 h		increases NPC1L1 expression	24904062
HepG2	Function Assay	0-25 μM	24 h		decreases subtilisin/kexin type 9 (PCSK9) protein levels dose dependently	24855646
HepG2	Function Assay	0-25 μM	24 h		increases low density lipoprotein receptor (LDLR) gene expression	24855646
HepG2	Function Assay	10 μm	0-24 h		decreases PCSK9 and HMGCR expression and increases LDLR expression after 6 h	24855646
HepG2	Function Assay	10 μm	24 h		promotes cytosolic neutral lipid accumulation independently of exogenous lipoproteins	24855646
HepG2	Function Assay	10 μm	24 h		prevents SREBP processing	24855646
HC45	Function Assay	5µM	4 d		reduces the methylation levels of WIF1, P16, CXCL14, NKX2–3, CDH1, LAMA1, and CTNNB1	24762809
CNDT2	Function Assay	5µM	4 d		reduces the methylation levels of WIF1, P16, CXCL14, NKX2–3, CDH1, LAMA1, and CTNNB1	24762809
CNDT2	Function Assay	5µM	4 d		increases gene expression of WIF1, P16, CDH1, LAMA1, and CTNNB1	24762809
T-cells	Growth Inhibition Assay	5/20 μM	0-48 h		inhibits cell growth in a dose dependent manner	24757283
CD3+ T-cells	Function Assay	5/20 μM	48 h		upregulates p15 expression	24757283
CD4+ T-cells	Function Assay	5/20 μM	48 h		upregulates p15 expression	24757283
CD8+ T-cells	Function Assay	5/20 μM	48 h		upregulates p15 expression	24757283
CD3+ T-cells	Function Assay	5/20 μM	48 h		upregulates the expression of FOXP3	24757283
CD4+ T-cells	Function Assay	5/20 μM	48 h		upregulates the expression of FOXP3	24757283
CD4+ T-cells	Function Assay	5/20 μM	48 h		reduces TBET1 mRNA expression	24757283
CD4+ T-cells	Function Assay	5/20 μM	48 h		upregulates the expression of RORγt	24757283
CD4+ T-cells	Function Assay	5/20 μM	48 h		inhibits memory T-cells	24757283
CD8+ T-cells	Function Assay	5/20 μM	48 h		inhibits memory T-cells	24757283
CD3+ T-cells	Function Assay	5 μM	48 h		reduces long-term memory cell phenotype	24757283
U937	Apoptosis Assay	10 μM	72 h		induces apoptosis significantly	24680865
HL-60	Apoptosis Assay	10 μM	72 h		induces apoptosis significantly	24680865
MCF7	Function Assay	5 μM	48 h		displays selective toxicity toward suspended MCF-7 cells	24633350
MCF7	Function Assay	10 μM	24 h		induces the cleavage of caspase 7 and PARP	24633350
MCF7	Function Assay	0–0.5 μM	7 d		inhibits the growth MCF-7 tumorspheres in suspension cultures	24633350
MCF7	Function Assay	0.5 μM	14 d		reduces the size of MCF-7 colonies embedded in soft agar	24633350
MCF7	Function Assay	0.05–20 μM	1 d		reduces the clonal survival of MCF-7 cells in monolayer cultures	24633350
T47D	Function Assay	0.5 μM	4 d		inhibits tumorsphere formation	24633350
MCF7	Function Assay	0.5–10 μM	48 h		inhibits the gap closure in the wound healing assay	24633350
MCF7	Function Assay	0/10 μM	24 h		inhibits the activity of MMP9	24633350
MDA-MB-231	Function Assay	0.5–10 μM	36 h		inhibits the migration	24633350
SKM1-S	Antiproliferative assay		48 hrs		Antiproliferative activity against human SKM1-S cells after 48 hrs by XTT assay, IC50 = 0.5 μM.	28094938
SKM1-S	Antiproliferative assay		48 hrs		Antiproliferative activity against human SKM1-S cells after 48 hrs by DAPI-staining-based flow cytometric method, EC50 = 0.51 μM.	28094938
A427	Antiproliferative assay		96 hrs		Antiproliferative activity against human A427 cells after 96 hrs by crystal violet assay, IC50 = 0.63 μM.	18434163
KYSE70	Antiproliferative assay		96 hrs		Antiproliferative activity against human KYSE70 cells after 96 hrs by crystal violet assay, IC50 = 1.59 μM.	18434163
5637	Antiproliferative assay		96 hrs		Antiproliferative activity against human 5637 cells after 96 hrs by crystal violet assay, IC50 = 1.73 μM.	18434163
HT-29	Antiproliferative assay		96 hrs		Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay, IC50 = 3.8 μM.	2778449
P388	Antiproliferative assay		48 hrs		Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay, IC50 = 5 μM.	2778449
MCF7	Antiproliferative assay		96 hrs		Antiproliferative activity against human MCF7 cells after 96 hrs by crystal violet assay, IC50 = 6.78 μM.	18434163
U373-MAGI	Antiviral assay	25 to 400 uM	2 to 72 hrs		Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in gag level at 25 to 400 uM after 2 to 72 hrs by qPCR method	27117260
U373-MAGI	Antiviral assay	25 to 400 uM	2 to 72 hrs		Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in U5-gag level at 25 to 400 uM after 2 to 72 hrs by qPCR method	27117260
L1210	Cytotoxicity assay				Cytotoxicity against mouse L1210 cells assessed as cessation of growth	69026
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
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
SKM1-S	Apoptosis assay	1 uM			Induction of apoptosis in human SKM1-S cells assessed as caspase 3 cleavage at 1 uM by Western blot method	28094938
MCF7	Function assay	15 uM	72 hrs		Inhibition of UHRF1 in human MCF7 cells assessed as decrease in methylation at RAR beta exon at 15 uM after 72 hrs by methylation specific-PCR method	27049577
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	244.2	Formule	C₈H₁₂N₄O₅	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	320-67-2	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	5-AzaC,Ladakamycin, AZA,5-Aza, CC-486,NSC 102816,5-Azacytidine			Smiles	C1=NC(=NC(=O)N1C2C(C(C(O2)CO)O)O)N

Solubilité (Solubility)

In vitro
Lot:

DMSO : 48 mg/mL (196.56 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Water : 50 mg/mL (超声加热五分钟)

DMSO : 48 mg/mL (196.56 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 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 30%PEG300 2 65%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	10.000mg/ml (40.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 650 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.
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	16% DMSO 1 84% saline Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	0.781mg/ml (3.20mM)	Taking the 1 mL working solution as an example, add 160 μL of 4.88 mg/ml clear DMSO stock solution to 840 μL of saline 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 l'expérience)

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

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y 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 d'abord 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 d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout 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 d'action (Mechanism of Action)

Targets/IC₅₀/Ki	DNA methyltransferase (Cell-free assay)
In vitro	L'azacitidine (5-Azacytidine) est largement utilisée pour démontrer la corrélation entre la perte de méthylation dans des régions géniques spécifiques et l'activation des gènes associés. Après incorporation dans l'ADN, elle inhibe l'ADN méthyltransférase de manière non compétitive, provoquant un blocage de la méthylation de la cytosine dans l'ADN nouvellement répliqué, mais pas dans les cellules au repos et non divisibles. Ce composé induit la différenciation des cellules d'érythroleucémie de Friend C3H10T1/2 avec formation de myotubes. Il peut être activé en nucléoside triphosphate et incorporé dans l'ADN et l'ARN, entraînant l'inhibition de la synthèse de l'ADN, de l'ARN et des protéines dans les cellules eucaryotes normales et dans les lignées cellulaires cancéreuses, ce qui peut finalement conduire à la mort cellulaire. L'azacitidine inhibe également l'incorporation des métabolites puriques dans les macromolécules. Elle inhibe la croissance des cellules L1210 avec une IC50 de 0,019 μg/mL.
In vivo	L'azacitidine (5-Azacytidine) inhibe la synthèse des polynucléotides chez les souris BDF₁ leucémiques. À une dose de 3 mg/kg (i.p.), elle augmente le temps de survie moyen chez les souris BDF1 leucémiques inoculées avec des cellules tumorales d'ascite Ll210. Ce composé supprime de manière marquée toute l'activité enzymatique de la voie de biosynthèse des polyamines, y compris l'activité de l'ornithine décarboxylase, l'activité de la S-adénosyl-L-méthionine décarboxylase dépendante de la putrescine et l'activité de la S-adénosyl-L-méthionine décarboxylase dépendante de la spermidine. Il inhibe également les accumulations de polyamines chez les souris leucémiques.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/12154409/ [2] https://pubmed.ncbi.nlm.nih.gov/6173384/ [3] https://pubmed.ncbi.nlm.nih.gov/5487063/ [4] https://pubmed.ncbi.nlm.nih.gov/4118428/

Applications (Applications)

Méthodes	Biomarqueurs	PMID
Western blot	DNMT1 c-PARP / p-H2AX / H2AX	28210112
Immunofluorescence	HMGB1	29097772
Growth inhibition assay	Cell viability	28210112

Informations sur l'essai clinique (Clinical Trial Information)

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

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT06372717	Not yet recruiting	Acute Myeloid Leukemia Refractory\|Myelodysplastic Syndrome Acute Myeloid Leukemia\|Myelodysplastic Syndrome With Excess Blasts\|Acute Myeloid Leukemia in Relapse	Apollo Therapeutics Ltd	April 2024	Phase 1\|Phase 2
NCT06263387	Not yet recruiting	AML Adult	French Innovative Leukemia Organisation\|Acute Leukemia French Association	April 29 2024	--
NCT06159491	Not yet recruiting	Chronic Myelomonocytic Leukemia	Douglas Tremblay\|Sobi Inc.\|Icahn School of Medicine at Mount Sinai	January 2 2024	Phase 1\|Phase 2
NCT06022003	Recruiting	AML Adult\|Refractory AML\|Relapsed Adult AML\|FLT3-TKD Mutation\|FLT3-ITD	French Innovative Leukemia Organisation\|Acute Leukemia French Association	January 13 2024	Phase 2
NCT06014489	Recruiting	AML Adult	Stichting Hemato-Oncologie voor Volwassenen Nederland	January 17 2024	Phase 2

Foire aux questions (Frequently Asked Questions)

Question 1:
Is the vehicle (30% Propylene glycol, 5% Tween 80, 65% D5W) for it (Catalog No.S1782) safe for subcutaneous dosing?

Réponse :
S1782 in 30% Propylene glycol+5% Tween 80+65% D5W at 30mg/ml is a suspension. If you are going to administrate this compound for oral gavage, it is fine. But if you administrate it via injection, you need a clear solution and it can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 10mg/ml clearly.

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):