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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)

N. Cat.: S1782

Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.

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

Struttura chimica

Peso molecolare: 244.2

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.92%

99.92

Prodotti spesso usati con 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.

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

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

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dell'attività	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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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	244.2	Formula	C₈H₁₂N₄O₅	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	320-67-2	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 48 mg/mL (196.56 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Water : 50 mg/mL (超声加热五分钟)

DMSO : 48 mg/mL (196.56 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

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.
Clear solution	5%DMSO 1 30%PEG300 2 65%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

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)

Targets/IC₅₀/Ki	DNA methyltransferase (Cell-free assay)
In vitro	L'azacitidina (5-Azacitidina) è ampiamente utilizzata per dimostrare la correlazione tra la perdita di metilazione in specifiche regioni geniche e l'attivazione dei geni associati. Dopo l'incorporazione nel DNA, inibisce la DNA metiltransferasi in modo non competitivo, causando un blocco della metilazione della citosina nel DNA appena replicato, ma non nelle cellule a riposo e non in divisione. Questo composto induce la differenziazione delle cellule di eritroleucemia di Friend C3H10T1/2 con formazione di miotubi. Può essere attivato a nucleoside trifosfato e incorporato sia nel DNA che nell'RNA, portando all'inibizione della sintesi di DNA, RNA e proteine nelle normali cellule eucariotiche e nelle linee cellulari tumorali, il che può infine portare alla morte cellulare. L'azacitidina inibisce anche l'incorporazione dei metaboliti purinici nelle macromolecole. Inibisce la crescita delle cellule L1210 con una IC50 di 0,019 μg/mL.
In vivo	L'azacitidina (5-Azacitidina) inibisce la sintesi di polinucleotidi nei topi BDF₁ leucemici. A una dose di 3 mg/kg (i.p.), aumenta il tempo medio di sopravvivenza nei topi BDF1 leucemici inoculati con cellule tumorali ascitiche Ll210. Questo composto sopprime marcatamente tutta l'attività enzimatica nella via biosintetica delle poliamine, inclusa l'attività dell'ornitina decarbossilasi, l'attività della S-adenosil-L-metionina decarbossilasi dipendente dalla putrescina e l'attività della S-adenosil-L-metionina decarbossilasi dipendente dalla spermidina. Inoltre, inibisce l'accumulo di poliamine nei topi leucemici.
Riferimenti	[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/

Applicazioni (Applications)

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

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Domande Frequenti (Frequently Asked Questions)

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

Risposta:
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):