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Réf. CatalogueS1896
| Cibles apparentées | HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Autre DNA/RNA Synthesis Inhibiteurs | CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279 Halofuginone |
| Lignées cellulaires | Type d'essai | Concentration | Temps d'incubation | Formulation | Description de l'activité | 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 | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 76.05 | Formule | CH4N2O2 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 127-07-1 | Télécharger le SDF | Stockage des solutions mères |
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| Synonymes | 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 |
|
In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| Targets/IC50/Ki |
ribonucleoside diphosphate reductase
|
|---|---|
| In vitro |
hydroxyurea peut inhiber la réplication du HIV-1. Des expériences in vitro ont montré que la concentration inhibitrice à 90 % (IC90) de ce composé pour les souches de laboratoire du HIV-1 dans les PBMC activées est de 0,4 mM. Il a également été trouvé synergique avec l'inhibiteur nucléosidique de la transcriptase inverse didanosine et pour inhiber la réplication du HIV-1 dans les PBMC activées ; cette inhibition peut être due à une réduction des tailles des pools de désoxynucléoside triphosphate. Il a été démontré que ce produit chimique sensibilise les mutants résistants à la didanosine. Il a démontré une activité dans le traitement de l'anémie falciforme en augmentant la production d'hémoglobine fœtale, ce qui réduit l'hémolyse chez les patients atteints de cette maladie. Cet agent exerce son effet cytostatique par l'inhibition de la ribonucléotide réductase - l'enzyme limitante responsable de la conversion des ribonucléotides en désoxyribonucléotides, qui sont essentiels à la synthèse de l'ADN. En conséquence, la division cellulaire est arrêtée en phase S.
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Références |
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(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| 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 |