solo para uso en investigación
Cat. No.: S1305
Estructura química
| Dianas relacionadas | HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Otros DNA/RNA Synthesis Inhibidores | CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Carmofur Triapine (3-AP) YK-4-279 Halofuginone |
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | 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 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
| Peso molecular | 152.18 | Fórmula | C5H4N4S |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 50-44-2 | Descargar SDF | Almacenamiento de soluciones madre |
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| Sinónimos | 6-MP | Smiles | C1=NC2=C(N1)C(=S)N=CN2 | ||
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In vitro |
DMSO
: 30 mg/mL
(197.13 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)
Resultados del cálculo:
Concentración de trabajo: mg/ml;
Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.
Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.
Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.
| 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. |
Referencias |
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(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)
| Número NCT | Reclutamiento | Condiciones | Patrocinador/Colaboradores | Fecha de inicio | Fases |
|---|---|---|---|---|---|
| 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 |