Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Hydroxyurea

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Hydroxyurea Ribonucleotide Reductase Inhibitor

Cat. No.: S1896

Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
Hydroxyurea DNA/RNA Synthesis inhibitor Chemical Structure

Estructura química

Peso molecular: 76.05

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.95%
99.95

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

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

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 76.05 Fórmula

CH4N2O2

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 127-07-1 Descargar SDF Almacenamiento de soluciones madre

Sinónimos NCI-C04831, Hydroxycarbamide,NSC-32065 Smiles C(=O)(N)NO

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 15 mg/mL (197.23 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : 15 mg/mL

Ethanol : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Mecanismo de acción (Mechanism of Action)

Targets/IC50/Ki
ribonucleoside diphosphate reductase
In vitro
hydroxyurea puede inhibir la replicación del HIV-1. Experimentos in vitro han demostrado que la concentración inhibitoria del 90% (IC90) de este compuesto para cepas de laboratorio de HIV-1 en PBMC activadas es de 0,4 mM. También se encontró que era sinérgico con el inhibidor de la transcriptasa inversa nucleósido didanosina y que inhibía la replicación del HIV-1 en PBMC activadas; esta inhibición puede deberse a una reducción en los tamaños de los grupos de desoxinucleósido trifosfato. Se ha demostrado que esta sustancia química sensibiliza a los mutantes resistentes a la didanosina. Ha demostrado actividad en el tratamiento de la anemia de células falciformes al aumentar la producción de hemoglobina fetal, lo que reduce la hemólisis en pacientes con esta enfermedad. Este agente ejerce su efecto citostático a través de la inhibición de la ribonucleótido reductasa, la enzima limitante de la velocidad responsable de la conversión de ribonucleótidos a desoxirribonucleótidos, que son esenciales para la síntesis de ADN. Como resultado, la división celular se detiene en la fase S.
Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/12101433/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT Reclutamiento Condiciones Patrocinador/Colaboradores Fecha de inicio Fases
NCT06171217 Recruiting
Sickle Cell Disease|Children
Children''s Hospital Medical Center Cincinnati|National Heart Lung and Blood Institute (NHLBI)
 October 27 2023 Phase 2
NCT05909657 Recruiting
Sickle Cell Disease
The University of The West Indies
 July 1 2023 --
NCT05548062 Recruiting
Polycythemia Vera
Novartis Pharmaceuticals|Novartis
 March 2 2023 --
NCT05662098 Recruiting
Sickle Cell Disease
Children''s Hospital Medical Center Cincinnati|Jinja Regional Referral Hospital (JRRH) Sickle Cell Clinic Jinja Uganda
 June 16 2022 Early Phase 1