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

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

Cat.Nr.S1782

Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486, NSC 102816) is een nucleoside-analoog van cytidine dat specifiek DNA methylation remt door DNA methyltransferases te vangen. Azacitidine induceert mitochondrial apoptosis en autophagy.

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

Chemische structuur

Moleculair gewicht: 244.2

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Kwaliteitscontrole

Batch: Zuiverheid: 99.92%

99.92

Producten Vaak Samen Gebruikt Met 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.

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

Celkweek, behandeling & werkconcentratie

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

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	244.2	Formule	C₈H₁₂N₄O₅	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	320-67-2	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 48 mg/mL (196.56 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Water : 50 mg/mL (超声加热五分钟)

DMSO : 48 mg/mL (196.56 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

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.
Clear solution	5%DMSO 1 30%PEG300 2 65%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste 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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste 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 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

Targets/IC₅₀/Ki	DNA methyltransferase (Cell-free assay)
In vitro	Azacitidine (5-Azacytidine) wordt veel gebruikt om de correlatie aan te tonen tussen het verlies van methylering in specifieke genregio's en de activering van de bijbehorende genen. Na incorporatie in DNA remt het DNA methyltransferase niet-competitief, wat een blokkering veroorzaakt in cytosine methylering in nieuw gerepliceerd DNA, maar niet in rustende, niet-delende cellen. Deze verbinding induceert differentiatie van Friend Erythroleukemia Cell C3H10T1/2 met myotubevorming. Het kan worden geactiveerd tot het nucleosidetrifosfaat en worden ingebouwd in zowel DNA als RNA, wat leidt tot remming van DNA-, RNA- en eiwitsynthese in normale eukaryote cellen en in kankercellijnen, wat uiteindelijk kan leiden tot celdood. Azacitidine remt ook de incorporatie van purinemetabolieten in macromoleculen. Het remt de groei van L1210-cellen met een IC50 van 0,019 μg/mL.
In vivo	Azacitidine (5-Azacytidine) remt de polynucleotidsynthese bij leukemische BDF₁-muizen. Bij een dosis van 3 mg/kg (i.p.) verhoogt het de gemiddelde overlevingstijd bij leukemische BDF1-muizen geïnoculeerd met Ll210 ascites tumorcellen. Deze verbinding onderdrukt alle enzymactiviteit in de polyamine-biosynthetische route aanzienlijk, inclusief ornithine decarboxylase-activiteit, putrescine-afhankelijke S-adenosyl-L-methionine decarboxylase-activiteit en spermidine-afhankelijke S-adenosyl-L-methionine decarboxylase-activiteit. Het remt ook de accumulatie van polyamines bij leukemische muizen.
Referenties	[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/

Toepassingen

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

Informatie klinische proef

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

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

Technische ondersteuning

Gebruiksaanwijzing

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

Als u nog andere vragen heeft, kunt u een bericht achterlaten.

Veelgestelde vragen

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

Antwoord:
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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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):