nur für Forschungszwecke
Kat.-Nr.S1200
| Verwandte Ziele | HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK |
|---|---|
| Weitere DNA Methyltransferase Inhibitoren | RG108 (N-Phthalyl-L-Tryptophan) SGI-1027 Zebularine (NSC 309132) GSK3685032 Gamma-Oryzanol β-thujaplicin CM272 Bobcat339 DC-05 2'-Deoxy-5-Fluorocytidine |
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| Eca109 | Function Assay | 0.5 μM | 24 h | water | modulates the gene expression of MAGE-A members | 25123082 |
| Eca109 | Growth Inhibition Assay | 0.5/2.5/5 μM | 24/48/72 h | water | inhibits cell growth in both dose- and time- dependent manner | 25123082 |
| Eca109 | Function Assay | 0.5 μM | 6/12/24 h | water | inhibits cell migration | 25123082 |
| Eca109 | Function Assay | 0.5 μM | 24 h | water | inhibits cell invasion | 25123082 |
| Eca109 | Growth Inhibition Assay | 0.5 μM | 24 h | water | induces G2/M arrest in the cell cycle | 25123082 |
| Eca109 | Function Assay | 0.5/1 μM | 24 h | water | decreases expression of NF-κB2 and MMP2 | 25123082 |
| SW1116 | Growth Inhibition Assay | 0.5/1/2/5 μM | 48 h | DMSO | enhances the Gefitinib induced cell inhibition | 24874286 |
| LOVO | Growth Inhibition Assay | 0.5/1/2/5 μM | 48 h | DMSO | enhances the Gefitinib induced cell inhibition | 24874286 |
| SW1116 | Function Assay | 10 μM | 48 h | DMSO | increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib | 24874286 |
| LOVO | Function Assay | 10 μM | 48 h | DMSO | increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib | 24874286 |
| SW1116 | Apoptosis Assay | 10 μM | 48 h | DMSO | enhances Gefitinib-induced apoptosis | 24874286 |
| LOVO | Apoptosis Assay | 10 μM | 48 h | DMSO | enhances Gefitinib-induced apoptosis | 24874286 |
| RPMI-8226 | Apoptosis Assay | 1/2 μM | 48/72/96 h | DMSO | induces cell apoptosis | 24833108 |
| OPM-2 | Apoptosis Assay | 1/2 μM | 72/96/120 h | DMSO | induces cell apoptosis | 24833108 |
| JJN3 | Apoptosis Assay | 0.5/1 μM | 24/48 h | DMSO | induces cell apoptosis | 24833108 |
| NCI-H929 | Apoptosis Assay | 1/2 μM | 72/96/120 h | DMSO | induces cell apoptosis | 24833108 |
| RPMI-8226 | Growth Inhibition Assay | 1/2 μM | 24/48/72 h | DMSO | affects cell cycle progression negatively | 24833108 |
| OPM-2 | Growth Inhibition Assay | 1/2 μM | 24/48/72 h | DMSO | affects cell cycle progression negatively | 24833108 |
| JJN3 | Growth Inhibition Assay | 0.5/1 μM | 24/48/72 h | DMSO | affects cell cycle progression negatively | 24833108 |
| NCI-H929 | Growth Inhibition Assay | 1/2 μM | 24/48/72 h | DMSO | affects cell cycle progression negatively | 24833108 |
| HeLa | Kinase Assay | Ki=1000–5000 μM for hENT1 | 24780098 | |||
| HeLa | Kinase Assay | Ki=5.6 ± 0.5 μM for hENT2 | 24780098 | |||
| HeLa | Kinase Assay | Ki=21.6 ± 3.0 μM for hCNT1 | 24780098 | |||
| HeLa | Kinase Assay | Ki=14.4 ± 4.6 μM for hCNT3 | 24780098 | |||
| NB4 | Function Assay | 2.5/5/7.5/10 μM | 24 h | DMSO | increasea the expression of precursor miR-125a | 24484870 |
| CD4+ CD25− T | Function Assay | 1/5 μM | reduceS global DNA methylation | 24476360 | ||
| BV-173 | Apoptosis Assay | 0.25/0.5/0.75/1 μM | 48/72/96 h | PBS | induces cell apoptosis in both dose- and time- dependent manner | 24423613 |
| ML-1 | Apoptosis Assay | 0.25/0.5/0.75/1 μM | 48/72/96 h | PBS | induces cell apoptosis in both dose- and time- dependent manner | 24423613 |
| HL-60 | Apoptosis Assay | 0.25/0.5/0.75/1 μM | 48/72/96 h | PBS | induces cell apoptosis in both dose- and time- dependent manner | 24423613 |
| KG-1a | Apoptosis Assay | 0.25/0.5/0.75/1 μM | 48/72/96 h | PBS | induces cell apoptosis in both dose- and time- dependent manner | 24423613 |
| BV-173 | Function Assay | 250/500nM | 48 h | PBS | induces delayed and sustained ROS increase | 24423613 |
| CEM | Function Assay | 250/500nM | 48 h | PBS | induces delayed and sustained ROS increase | 24423613 |
| HL-60 | Function Assay | 250/500nM | 48 h | PBS | induces delayed and sustained ROS increase | 24423613 |
| ML-1 | Function Assay | 250/500nM | 48 h | PBS | induces delayed and sustained ROS increase | 24423613 |
| DLD-1 | Function Assay | 250/500nM | 48 h | PBS | do not induces delayed and sustained ROS increase | 24423613 |
| HCT-116 | Function Assay | 250/500nM | 48 h | PBS | do not induces delayed and sustained ROS increase | 24423613 |
| U937-A/E-9/14/18 | Apoptosis Assay | 0.01/0.1/1/10 μM | 48 h | induces cell apoptosis in a dose-dependent manner | 24300456 | |
| HT29 | Growth Inhibition Assay | 72 h | IC50=1400±179 μM | 24172061 | ||
| SW48 | Growth Inhibition Assay | 72 h | IC50=15.2±6.2 μM | 24172061 | ||
| HCT116 | Growth Inhibition Assay | 72 h | IC50=1.7±0.4 μM | 24172061 | ||
| HepG2 | Function Assay | 0.5/1 μM | 24 h | DMSO | up-regulated the relative OCTN2 mRNA and protein expression | 24146874 |
| LS174T | Function Assay | 0.5/1 μM | 24 h | DMSO | lead to an increase of OCTN2 levels | 24146874 |
| HepG2 | Apoptosis Assay | 1/10/100 μM | 7 d | DMSO | induces cell apoptosis in a dose-dependent manner | 24146874 |
| LS174T | Apoptosis Assay | 1/10/100 μM | 7 d | DMSO | induces cell apoptosis in a dose-dependent manner | 24146874 |
| QBC-939 | Apoptosis Assay | 1/10/100 μM | 7 d | DMSO | induces cell apoptosis in a dose-dependent manner | 24146874 |
| U251 | Apoptosis Assay | 1/10/100 μM | 7 d | DMSO | induces cell apoptosis in a dose-dependent manner | 24146874 |
| HL-60 | Growth Inhibition Assay | 1 μM | 48 h | increases G2-phase cell fraction | 24000324 | |
| MDA‑MB‑453 | Function Assay | 0.2/1 μM | 72 h | causes re-expression of claudin 1 | 23844228 | |
| HCC1569 | Function Assay | 0.2/1 μM | 72 h | causes re-expression of claudin 1 | 23844228 | |
| BT‑474 | Function Assay | 0.2/1 μM | 72 h | causes re-expression of claudin 1 | 23844228 | |
| AGS | Apoptosis Assay | 5/10/20/50 μM | 48 h | DMSO | inhibits the cell viability | 23582784 |
| A549 | Apoptosis Assay | 5/10/20/50 μM | 48 h | DMSO | inhibits the cell viability | 23582784 |
| AGS | Growth Inhibition Assay | 5/10/20/50 μM | 48 h | DMSO | induces G2/M phase arrest | 23582784 |
| Kasumi-1 | Apoptosis Assay | 0.5 μM | 48 h | decreases the cell viability co-treated with Tf-NP-sc | 23493348 | |
| OCI-AML3 | Apoptosis Assay | 2.5 μM | 48 h | decreases the cell viability co-treated with Tf-NP-sc | 23493348 | |
| MV4-11 | Apoptosis Assay | 2.5 μM | 48 h | decreases the cell viability co-treated with Tf-NP-sc | 23493348 | |
| NK | Cytotoxity Assay | 0.02-20 μM | 5 d | decreases the cytolytic activity of NK cells at intermediate concentrations resulting in a U-shaped dose–response curve | 23328088 | |
| NK | Apoptosis Assay | 0.02-20 μM | 5 d | decrease NK cell proliferation and viability as the concentration increased | 23328088 | |
| NK | Function Assay | 0.01-20 μM | 5 d | causes hypomethylation of NK cells in a dose–response | 23328088 | |
| MOLT4/DNR | Function Assay | 5 μM | 4 d | reduces ABCB1 mRNA expression | 23060570 | |
| Jurkat/DOX | Function Assay | 5 μM | 4 d | reduces ABCB1 mRNA expression | 23060570 | |
| MOLT4/DNR | Growth Inhibition Assay | 5 μM | 4 d | reduces the IC50 value for daunorubicin sensitivity | 23060570 | |
| Jurkat/DOX | Growth Inhibition Assay | 5 μM | 4 d | reduces the IC50 value for daunorubicin sensitivity | 23060570 | |
| ccRCC | Apoptosis Assay | 0.01-10μM | 72 h | DMSO | has minimal effect on cell proliferation | 22826467 |
| TNBC | Apoptosis Assay | 0.01-10μM | 72 h | DMSO | has minimal effect on cell proliferation | 22826467 |
| A498 | Apoptosis Assay | 0.01-10μM | 72 h | DMSO | induces synergistic responses with romidepsin | 22826467 |
| KIJ265T | Apoptosis Assay | 0.01-10μM | 72 h | DMSO | induces synergistic responses with romidepsin | 22826467 |
| MDA-231 | Apoptosis Assay | 0.01-10μM | 72 h | DMSO | induces synergistic responses with romidepsin | 22826467 |
| BT-20 | Apoptosis Assay | 0.01-10μM | 72 h | DMSO | induces synergistic responses with romidepsin | 22826467 |
| U937 | Growth Inhibition Assay | 5-20 μM | 24/48/72 h | induces a decrease in cell viability in a concentration- and time-dependent manner | 22767021 | |
| HL60 | Growth Inhibition Assay | 5-20 μM | 24/48/72 h | induces a decrease in cell viability in a concentration- and time-dependent manner | 22767021 | |
| U937 | Apoptosis Assay | 15 μM | 24/48/72 h | induces cell apoptosis | 22767021 | |
| HL60 | Apoptosis Assay | 15 μM | 24/48/72 h | induces cell apoptosis | 22767021 | |
| LS411N | Apoptosis Assay | 0.5 μM | 72 h | increases Fas mRNA level | 22461695 | |
| MDA-MB-231 | Apoptosis Assay | 10 μM | 48 h | reduces cell viability in a dose-dependent manner | 21887697 | |
| MCF-7 | Apoptosis Assay | 10 μM | 48 h | reduces cell viability in a dose-dependent manner | 21887697 | |
| A375 | Growth Inhibition Assay | 0.5 μM | 1/5/8 d | inhibits proliferation and induces differentiation of melanoma cells | 21796622 | |
| SKMEL1 | Growth Inhibition Assay | 0.5 μM | 1/5/8 d | inhibits proliferation and induces differentiation of melanoma cells | 21796622 | |
| SKMEL3 | Growth Inhibition Assay | 0.5 μM | 1/5/8 d | inhibits proliferation and induces differentiation of melanoma cells | 21796622 | |
| SKMEL28 | Growth Inhibition Assay | 0.5 μM | 1/5/8 d | inhibits proliferation and induces differentiation of melanoma cells | 21796622 | |
| MeWo | Growth Inhibition Assay | 0.5 μM | 1/5/8 d | inhibits proliferation and induces differentiation of melanoma cells | 21796622 | |
| B16 | Growth Inhibition Assay | 0.5 μM | 1/5/8 d | inhibits proliferation and induces differentiation of melanoma cells | 21796622 | |
| Ly 1 | Growth Inhibition Assay | 24 h | IC50=7.3 μM | 21772049 | ||
| Ly 7 | Growth Inhibition Assay | 24 h | IC50=10.7 μM | 21772049 | ||
| Su-DHL6 | Growth Inhibition Assay | 24 h | IC50>20 μM | 21772049 | ||
| Ly 10 | Growth Inhibition Assay | 24 h | IC50>20 μM | 21772049 | ||
| RIVA | Growth Inhibition Assay | 24 h | IC50>20 μM | 21772049 | ||
| Su-DHL2 | Growth Inhibition Assay | 24 h | IC50>20 μM | 21772049 | ||
| Ly 1 | Growth Inhibition Assay | 48 h | IC50=0.34 μM | 21772049 | ||
| Ly 7 | Growth Inhibition Assay | 48 h | IC50=0.025 μM | 21772049 | ||
| Su-DHL6 | Growth Inhibition Assay | 48 h | IC50>20 μM | 21772049 | ||
| Ly 10 | Growth Inhibition Assay | 48 h | IC50=1.8 μM | 21772049 | ||
| RIVA | Growth Inhibition Assay | 48 h | IC50>20 μM | 21772049 | ||
| Su-DHL2 | Growth Inhibition Assay | 48 h | IC50=17.4 μM | 21772049 | ||
| Ly 1 | Growth Inhibition Assay | 72 h | IC50=0.01 μM | 21772049 | ||
| Ly 7 | Growth Inhibition Assay | 72 h | IC50=0.018 μM | 21772049 | ||
| Su-DHL6 | Growth Inhibition Assay | 72 h | IC50=1.6 μM | 21772049 | ||
| Ly 10 | Growth Inhibition Assay | 72 h | IC50=1.2 μM | 21772049 | ||
| RIVA | Growth Inhibition Assay | 72 h | IC50>20 μM | 21772049 | ||
| Su-DHL2 | Growth Inhibition Assay | 72 h | IC50=11.2 μM | 21772049 | ||
| U373-MAGI | Antiviral assay | 0.25 to 8 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 0.25 to 8 uM after 2 to 72 hrs by qPCR method | 27117260 | |
| U373-MAGI | Antiviral assay | 0.25 to 8 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 0.25 to 8 uM after 2 to 72 hrs by qPCR method | 27117260 | |
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
| Molekulargewicht | 228.21 | Formel | C8H12N4O4 |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 2353-33-5 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716 | Smiles | C1C(C(OC1N2C=NC(=NC2=O)N)CO)O | ||
|
In vitro |
DMSO
: 45 mg/mL
(197.18 mM)
Water : 22.5 mg/mL Ethanol : Insoluble |
|
In vivo |
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Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
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.)
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.
| Targets/IC50/Ki |
DNA methylation
(HL-60, KG1a cells) |
|---|---|
| In vitro |
Decitabine hemmt das Zellwachstum dosis- und zeitabhängig mit einem IC50 von ungefähr 438 nM und 43,8 nM bei einer Exposition von 72 Stunden bzw. 96 Stunden in HL-60- und KG1a-Leukämiezellen. Eine aktuelle Studie zeigt, dass diese Verbindung eine hohe antiproliferative und pro-apoptotische Aktivität gegen anaplastisches großzelliges Lymphom (ALCL) aufweist und die [3H]–Thymidin-Aufnahme in KARPAS-299-Zellen mit einem EC50 von 0,49 μM hemmt. |
| Kinase-Assay |
DNA synthesis assay
|
|
Die Rate der DNA-Synthese wird durch den Einbau von radioaktivem Thymidin in die DNA gemessen. HL-60- und KG1a-Zellen werden in 2 ml RPMI-Medium, das 10% fetales Serum enthält, in 6-Well-Schalen (35 mm Durchmesser) suspendiert und 48 Stunden lang mit verschiedenen Konzentrationen der entsprechenden Medikamente inkubiert (Medikamente werden gleichzeitig hinzugefügt). Nach 48 Stunden werden 0,5 μCi [3H]-Thymidin (6,7 Ci/mmol) zu jedem Well hinzugefügt und weitere 24 Stunden inkubiert. Die Zellen werden auf GF/C-Glasfaserfiltern (2,4 cm Durchmesser) platziert, mit kaltem 0,9% NaCl, 5% kalter Trichloressigsäure und Ethanol gewaschen. Die DNA enthaltenden Filter werden dann getrocknet, in EcoLite-Szintillationsflüssigkeit (ICN) gegeben und die Radioaktivität mit einem Beckman LS 6000IC-Szintillationszähler gemessen. Der IC50 ist definiert als die Medikamentenkonzentration, die 50% der DNA-Synthese der Leukämiezelllinien aus der Dosis-Wirkungs-Kurve hemmt.
|
|
| In vivo |
In einem ALK+ KARPAS-299 Maus-Xenograft-Modell bewirkt Decitabine in einer Dosis von 2,5 mg/kg eine erhöhte Apoptose und eine reduzierte Proliferation der Tumorzellen, und führt auch zur Demethylierung des Tumorsuppressorgens p16INK4A. |
Literatur |
|
| Methoden | Biomarker | Bilder | PMID |
|---|---|---|---|
| Western blot | Survivin / Bcl-2 / p53 / c-Myc / DNMT1 p-AKT / AKT / p-GSK3β / GSK3β / p-Myc / Myc / p-P70 / P70 / p-4EBP-1 / 4EBP-1 / PTEN phospho-p38 / p38 / phospho-NFκB / NFκB p-JAK1 / JAK1 / p-JAK2 / JAK2 / p-STAT3 / STAT3 E-cadherin / N-cadherin / Snail / MMP-2 / MMP-9 / Bcl-2 / Bax |
|
26384351 |
| Immunofluorescence | DNMT1 E-cadherin / MMP-9 |
|
21303982 |
| Growth inhibition assay | Cell viability |
|
26384351 |
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| NCT06291285 | Not yet recruiting | Healthy Volunteers |
Novo Nordisk A/S |
February 27 2024 | Phase 1 |
| NCT05960773 | Recruiting | Mesothelioma|Malignant Mesothelioma (MM)|Early-stage Mesothelioma|Subclinical Mesothelioma|BRCA1-Associated Protein-1 (BAP1) Mutations|Early-stage BAP1-associated Malignancies |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
January 31 2024 | Phase 2 |
| NCT05835011 | Terminated | Myelodysplastic Syndromes |
Astex Pharmaceuticals Inc. |
July 14 2023 | Phase 2 |
| NCT05816356 | Recruiting | Healthy |
EpiDestiny Inc.|Worldwide Clinical Trials |
March 24 2023 | Phase 1 |
Frage 1:
Is it a racemic mixture or a monomer?
Antwort:
Its S1200 is R form.