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

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

Kat.-Nr.S1782

Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) ist ein Nucleosid-Analogon von Cytidin, das spezifisch die DNA methylation durch Einfangen von DNA Methyltransferase hemmt. Azacitidine induziert mitochondriale Apoptose und Autophagy.

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

Chemische Struktur

Molekulargewicht: 244.2

Springe zu

Qualitätskontrolle

Charge: Reinheit: 99.92%

99.92

Produkte, die oft zusammen verwendet werden mit 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.

Verwandte Ziele	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Weitere DNA Methyltransferase Inhibitoren	RG108 SGI-1027 Zebularine (NSC 309132) GSK3685032 Gamma-Oryzanol CM272 β-thujaplicin Bobcat339 DC-05 2'-Deoxy-5-Fluorocytidine

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Formulierung	Aktivitätsbeschreibung	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
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität

Molekulargewicht	244.2	Formel	C₈H₁₂N₄O₅	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	320-67-2	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	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

Löslichkeit

In vitro
Charge:

DMSO : 48 mg/mL (196.56 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 49 mg/mL (200.65 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 48 mg/mL (196.56 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 48 mg/mL (196.56 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Water : 50 mg/mL (超声加热五分钟)

DMSO : 48 mg/mL (196.56 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : Insoluble

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
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 Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	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 Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	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.

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Targets/IC₅₀/Ki	DNA methyltransferase (Cell-free assay)
In vitro	Azacitidine (5-Azacytidine) wird häufig verwendet, um die Korrelation zwischen dem Verlust der Methylierung in spezifischen Genregionen und der Aktivierung der zugehörigen Gene nachzuweisen. Nach der Incorporation in die DNA hemmt es die DNA Methyltransferase nichtkompetitiv, was zu einer Blockierung der Cytosinmethylierung in neu replizierter DNA führt, jedoch nicht in ruhenden, nicht-teilenden Zellen. Diese Verbindung induziert die Differenzierung von Friend Erythroleukämie-Zellen C3H10T1/2 mit Myotubenbildung. Es kann zu Nucleosid-Triphosphat aktiviert und sowohl in DNA als auch in RNA eingebaut werden, was zu einer Hemmung der DNA-, RNA- und Proteinsynthese in normalen eukaryotischen Zellen und in Krebszelllinien führt, was schließlich zum Zelltod führen kann. Azacitidine hemmt auch die Incorporation von Purinmetaboliten in Makromoleküle. Es hemmt das Wachstum von L1210-Zellen mit einem IC50-Wert von 0,019 μg/mL.
In vivo	Azacitidine (5-Azacytidine) hemmt die Polynucleotidsynthese in leukämischen BDF₁-Mäusen. Bei einer Dosis von 3 mg/kg (i.p.) erhöht es die mittlere Überlebenszeit bei leukämischen BDF1-Mäusen, die mit Ll210-Aszites-Tumorzellen inokuliert wurden. Diese Verbindung unterdrückt alle Enzymaktivitäten im Polyamin-biosynthetischen Weg erheblich, einschließlich der Ornithin-Decarboxylase-Aktivität, der Putrescin-abhängigen S-Adenosyl-L-Methionin-Decarboxylase-Aktivität und der Spermidin-abhängigen S-Adenosyl-L-Methionin-Decarboxylase-Aktivität. Es hemmt auch die Akkumulation von Polyaminen in leukämischen Mäusen.
Literatur	[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/

Anwendungen

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

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
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

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Häufig gestellte Fragen

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

Antwort:
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.

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