nur für Forschungszwecke
Kat.-Nr.: S1305
Chemische Struktur
| Verwandte Ziele | HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Weitere DNA/RNA Synthesis Inhibitoren | CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Carmofur Triapine (3-AP) YK-4-279 Halofuginone |
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| L1210 leukemia cells | Function assay | Inhibitory concentration on multidrug-resistant L1210 leukemia cells, IC50=0.024 μM | ||||
| MT4 cells | Proliferation assay | Antiproliferative activity against human MT4 cells by MTT assay, IC50=0.1 μM | ||||
| human CCRF-CEM cells | Proliferation assay | Antiproliferative activity against human CCRF-CEM cells by MTT assay, IC50=1 μM | ||||
| human CCRF-SB cells | Proliferation assay | Antiproliferative activity against human CCRF-SB cells by MTT assay, IC50=1 μM | ||||
| human SK-MEL-28 cells | Proliferation assay | Antiproliferative activity against human SK-MEL-28 cells by MTT assay, IC50=15 μM | ||||
| human MCF7 cells | Proliferation assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50=3 μM | ||||
| human HepG2 cells | Proliferation assay | Antiproliferative activity against human HepG2 cells by MTT assay, IC50=8 μM | ||||
| human DU145 cells | Proliferation assay | Antiproliferative activity against human DU145 cells by MTT assay, IC50=2 μM | ||||
| mouse J774.A1 cells | Proliferation assay | 3 days | Antiproliferative activity against mouse J774.A1 cells after 3 days by MTT conversion assay, IC50=0.003 μM | |||
| HEK293 cells | Proliferation assay | 3 days | Antiproliferative activity against HEK293 cells after 3 days by MTT conversion assay, IC50=0.007 μM | |||
| mouse J774 cells | Proliferation assay | 72 h | Antiproliferative activity against mouse J774 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.003 μM | |||
| human PBMC | Function assay | 4 days | Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days, IC50=0.1495 μM | |||
| HeLa cells | Cytotoxicity assay | 48 h | Cytotoxicity against human HeLa cells at lag phase of growth after 48 hrs by MTT assay, IC50=2.9 μM | |||
| A549 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A549 cells at lag phase of growth after 48 hrs by MTT assay, IC50=47 μM | |||
| MCF7 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human MCF7 cells at lag phase of growth after 48 hrs by MTT assay, IC50=1.4 μM | |||
| MT4 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human MT4 cells infected with HTLV-1 after 96 hrs by MTT assay, CC50=0.1 μM | |||
| CCRF-CEM cells | Proliferation assay | 96 h | Antiproliferative activity against human CCRF-CEM cells after 96 hrs by MTT assay, CC50=1 μM | |||
| WIL2-NS cells | Proliferation assay | 96 h | Antiproliferative activity against human WIL2-NS cells after 96 hrs by MTT assay, CC50=3 μM | |||
| CCRF-SB cells | Proliferation assay | 96 h | Antiproliferative activity against human CCRF-SB cells after 96 hrs by MTT assay, CC50=1.1 μM | |||
| human DU145 cells | Proliferation assay | 96 h | Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, CC50=2 μM | |||
| human HepG2 cells | Proliferation assay | 96 h | Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, CC50=8 μM | |||
| MCF7 cells | Proliferation assay | 96 h | Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, CC50=3.2 μM | |||
| SK-MEL-28 cells | Proliferation assay | 96 h | Antiproliferative activity against human SK-MEL-28 cells after 96 hrs by MTT assay, CC50=15 μM | |||
| MCF7 cells | Cytotoxicity assay | Cytotoxicity against human MCF7 cells, IC50=2.79 μM | ||||
| mouse S49 cells | Cytotoxicity assay | 72 h | Cytotoxicity against wild type mouse S49 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay, EC50=8 μM | |||
| Colo-357 cells | Cytotoxicity assay | Cytotoxicity against human Colo-357 cells by crystal violet staining, IC50=6.12 μM | ||||
| Aspc-1 cells | Cytotoxicity assay | Cytotoxicity against human Aspc-1 cells by crystal violet staining, IC50=2.45 μM | ||||
| A549 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=47 μM | |||
| MCF7 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50=1.4 μM | |||
| Patu-02 cells | Cytotoxicity assay | Cytotoxicity against human Patu-02 cells by crystal violet staining, IC50=9.69 μM | ||||
| Patu-T cells | Cytotoxicity assay | Cytotoxicity against human Patu-T cells by crystal violet staining, IC50=4.09 μM | ||||
| Patu-S cells | Cytotoxicity assay | Cytotoxicity against human Patu-S cells by crystal violet staining, IC50=11.07 μM | ||||
| T3M4 cells | Cytotoxicity assay | Cytotoxicity against human T3M4 cells by crystal violet staining, IC50=2.63 μM | ||||
| human PANC1 cells | Cytotoxicity assay | Cytotoxicity against human PANC1 cells by crystal violet staining, IC50=6.39 μM | ||||
| human DAN-G cells | Cytotoxicity assay | Cytotoxicity against human DAN-G cells by crystal violet staining, IC50=4.06 μM | ||||
| HeLa cells | Cytotoxicity assay | 48 h | Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50=2.9 μM | |||
| WEHI164 cells | Proliferation assay | 3 days | Antiproliferative activity against mouse WEHI164 cells after 3 days by MTT conversion assay, IC50=0.015 μM | |||
| WIL-2NS cells | Proliferation assay | Antiproliferative activity against human WIL-2NS cells by MTT assay, IC50=3 μM | ||||
| WEHI164 cells | Proliferation assay | 72 h | Antiproliferative activity against mouse WEHI164 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.017 μM | |||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
| Molekulargewicht | 152.18 | Formel | C5H4N4S |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 50-44-2 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | 6-MP | Smiles | C1=NC2=C(N1)C(=S)N=CN2 | ||
|
In vitro |
DMSO
: 30 mg/mL
(197.13 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
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 |
PRPP Amidotransferase
|
|---|---|
| In vitro |
Mercaptopurine (6-MP) is widely used to treat malignancies, rheumatic diseases, dermatologic conditions, inflammatory bowel disease, and solid organ transplant rejection. It inhibits purine nucleotide synthesis and metabolism by inhibiting an enzyme called Phosphoribosyl pyrophosphate amidotransferase (PRPP Amidotransferase). PRPP Amidotransferase is the rate limiting enzyme of purine synthesis. This compound alters the synthesis and function of RNA and DNA. It interferes with nucleotide interconversion and glycoprotein synthesis. |
Literatur |
|
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| NCT04770922 | Completed | Acute Lymphoblastic Leukemia Pediatric|Adverse Drug Event |
Cipherome Inc.|Stanford University |
February 23 2021 | -- |
| NCT03022747 | Unknown status | Lymphoblastic Leukemia Acute Childhood |
Vastra Gotaland Region |
January 2017 | Phase 2 |