solo para uso en investigación
Cat. No.: S1896
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) RK-33 EED226 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 | Growth inhibition assay | Concentration required for 50% inhibition of cell growth (L1210 Leukemia), IC50=21.3796 μM | 2991520 | |||
| P388 leukemic cell | Proliferation assay | 24-48 h | Antiproliferative activity of compound expressed as concentration that inhibits 50% of growth of P388 leukemic cell suspension from 24 to 48 hr after compound addition, IC50=32 μM | 2709372 | ||
| L1210 | Function assay | 48 h | Activity against cultured L1210 leukemic cells was determined in vitro, after 48 h of incubation. Compound dose that causes 16 % inhibition was reported, ID16 = 1.99 μM. | 6319702 | ||
| U373-MAGI | Function assay | 500 uM | 2 hrs | Potentiation of 5-Aza-C-induced antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as 5-Aza-C EC50 at 500 uM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs and subsequent viral infection meas, EC50 = 25.8 μM. | 27117260 | |
| Burkitt's lymphoma cells | Function assay | Inhibition of [14C]-cytidine incorporation into DNA in Burkitt's lymphoma cells, IC50 = 37.15 μM. | 11405653 | |||
| U373-MAGI | Antiviral assay | 500 uM | Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in viral infectivity at 500 uM incubated for 4 hrs prior to viral infection measured at 72 hrs post infection by flow cytometric analysis | 27117260 | ||
| U373-MAGI | Function assay | 0.5 mM | 2 hrs | Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 0.5 mM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-C | 27117260 | |
| U373-MAGI | Function assay | 2 mM | 6 hrs | Reduction in dATP level in human U373-MAGI cells at 2 mM after 6 hrs by LC-MS/MS analysis | 27117260 | |
| U373-MAGI | Function assay | 0.5 mM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 0.5 mM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis | 27117260 | |
| U373-MAGI | Function assay | 2 mM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 2 mM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-C | 27117260 | |
| U373-MAGI | Function assay | 0.5 mM | 2 hrs | Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 0.5 mM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 | |
| U373-MAGI | Function assay | 2 mM | 2 hrs | Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 2 mM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 | |
| U373-MAGI | Function assay | 0.5 mM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 0.5 mM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 | |
| U373-MAGI | Function assay | 2 mM | 2 hrs | Reduction in dCTP level in human U373-MAGI cells at 2 mM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC | 27117260 | |
| 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 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) 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 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
| Peso molecular | 76.05 | Fórmula | CH4N2O2 |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 127-07-1 | Descargar SDF | Almacenamiento de soluciones madre |
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| Sinónimos | NCI-C04831, Hydroxycarbamide,NSC-32065 | Smiles | C(=O)(N)NO | ||
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In vitro |
DMSO
: 15 mg/mL
(197.23 mM)
Water : 15 mg/mL Ethanol : Insoluble |
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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 |
ribonucleoside diphosphate reductase
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|---|---|
| In vitro |
hydroxyurea can inhibit HIV-1 replication. In vitro experiments have shown that the 90% inhibitory concentration (IC90) of this compound for laboratory strains of HIV-1 in activated PBMC is 0.4 mM. It was also found to be synergistic with the nucleoside reverse transcriptase inhibitor didanosine and to inhibit HIV-1 replication in activated PBMC; this inhibition may be due to a reduction in deoxynucleoside triphosphate pool sizes. This chemical has been shown to sensitize didanosine-resistant mutants. It has demonstrated activity in the treatment of sickle cell anemia by increasing the production of fetal hemoglobin, which reduces hemolysis in patients with this disease. This agent exerts its cytostatic effect through inhibition of ribonucleotide reductase—the rate-limiting enzyme responsible for the conversion of ribonucleotides to deoxyribonucleotides, which are essential for DNA synthesis. As a result, cellular division is arrested in the S phase.
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Referencias |
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(datos de https://clinicaltrials.gov, actualizado el 2026-07-23)
| Número NCT | Reclutamiento | Condiciones | Patrocinador/Colaboradores | Fecha de inicio | Fases |
|---|---|---|---|---|---|
| NCT07616154 | RECRUITING | Sickle Cell Disease |
St. Jude Children's Research Hospital |
2026-09 | PHASE2 |
| NCT07722611 | NOT_YET_RECRUITING | Polycythemia Vera |
Merck Sharp & Dohme LLC |
2026-09-21 | PHASE2; PHASE3 |
| NCT07708714 | RECRUITING | Sickle Cell Disease; Sickle Cell Anemia in Children |
Children's Hospital Medical Center, Cincinnati |
2026-05-13 | PHASE1; PHASE2 |
| NCT06526117 | RECRUITING | Sickle Cell Disease; Stroke |
Vanderbilt University Medical Center |
2024-08-05 | PHASE4 |
| NCT06439082 | RECRUITING | Sickle Cell Disease |
Novartis Pharmaceuticals |
2024-10-24 | PHASE3 |
| NCT07766850 | NOT_YET_RECRUITING | R/R AML |
Christer C Nilsson |
2026-10 | PHASE1; PHASE2 |