Name: Hydroxyurea
Brand: Selleck Chemicals
SKU: S1896
Rating: 5 (52 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.95%

99.95

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF
Overige DNA/RNA Synthesis Inhibitoren	CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279 Halofuginone

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	76.05	Formule	CH₄N₂O₂	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	127-07-1	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NCI-C04831, Hydroxycarbamide,NSC-32065			Smiles	C(=O)(N)NO

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 15 mg/mL (197.23 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 15 mg/mL

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	ribonucleoside diphosphate reductase
In vitro	Hydroxyurea kan HIV-1-replicatie remmen. In vitro-experimenten hebben aangetoond dat de 90% remmende concentratie (IC90) van deze verbinding voor laboratoriumstammen van HIV-1 in geactiveerde PBMC 0,4 mM is. Er werd ook vastgesteld dat het synergetisch werkt met de nucleoside reverse transcriptase-remmer didanosine en dat het de HIV-1-replicatie in geactiveerde PBMC remt; deze remming kan te wijten zijn aan een vermindering van de deoxynucleosidetrifosfaat-poolgroottes. Van deze chemische stof is aangetoond dat het didanosine-resistente mutanten gevoelig maakt. Het heeft activiteit aangetoond bij de behandeling van sikkelcelanemie door de productie van foetaal hemoglobine te verhogen, wat hemolyse vermindert bij patiënten met deze ziekte. Dit middel oefent zijn cytostatische effect uit door remming van ribonucleotide reductase - het snelheidsbeperkende enzym dat verantwoordelijk is voor de omzetting van ribonucleotiden naar deoxyribonucleotiden, die essentieel zijn voor DNA synthesis. Als gevolg hiervan wordt de celdeling gearresteerd in de S-fase
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/10860905/ [2] https://pubmed.ncbi.nlm.nih.gov/10860899/ [3] https://pubmed.ncbi.nlm.nih.gov/16338491/ [4] https://pubmed.ncbi.nlm.nih.gov/12101433/

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

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C8=C7/X	C8:	LOG(C8):

Hydroxyurea Ribonucleotide Reductase Inhibitor

Chemische structuur

Moleculair gewicht: 76.05

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie klinische proef (Clinical Trial Information)

Hydroxyurea Ribonucleotide Reductase Inhibitor

Chemische structuur

Moleculair gewicht: 76.05

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie klinische proef (Clinical Trial Information)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)