Hydroxyurea (Hydroxycarbamide)

Alias: NCI-c04831; NSC-32065; NCI c04831; NSC 32065; NCIc04831; NSC32065; Biosupressin; Carbamoyl oxime; Droxia; Hydroxycarbamide

Cat No.:V1464 Purity: ≥98%

COA Product Data Instructions for use SDS

Hydroxyurea (Hydroxycarbamide) Chemical Structure CAS No.: 127-07-1
Product category: DNA(RNA) Synthesis

This product is for research use only, not for human use. We do not sell to patients.

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Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Nature 597, 119–125 (2021)

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Hydroxyurea (formerly known as NCI-c04831, NSC-32065; NCIc04831, NSC32065; Biosupressin; Carbamoyl oxime; Droxia; Hydroxycarbamide) is an approved antineoplastic drug that has been used for treating various cancers such as melanoma, sickle-cell disease and resistant chronic myelocytic leukemia. Through the inhibition of ribonucleoside diphosphate reductase, it inhibits DNA synthesis and induces cell death. A hydroxyurea may prevent HIV-1 from replicating. The 90% inhibitory concentration (IC90) of hydroxyurea for laboratory strains of HIV-1 in activated PBMC has been demonstrated by in vitro experiments to be 0.4 mM.

Biological Activity I Assay Protocols (From Reference)

Targets

HIV-1

ln Vitro

Hydroxyurea can inhibit HIV-1 replication. The 90% inhibitory concentration (IC90) of hydroxyurea for laboratory strains of HIV-1 in activated PBMC has been demonstrated by in vitro experiments to be 0.4 mM. In activated PBMC, hydroxyurea was also found to inhibit HIV-1 replication and work in concert with didanosine, a nucleoside reverse transcriptase inhibitor; this inhibition may be brought about by a decrease in the amounts of deoxynucleoside triphosphate pools. Mutants resistant to didanosine have been shown to become sensitized to hydroxyurea[1][2]. In sickle cell anemia patients, hydroxyurea has been shown to be effective in reducing hemolysis by boosting the fetal hemoglobin production. Ribonucleotide reductase is the rate-limiting enzyme that converts ribonucleotides into deoxyribonucleotides, which are necessary for DNA synthesis. Hydroxyurea inhibits this enzyme to produce its cytostatic effect. Consequently, the S phase of cellular division is halted[1].

ln Vivo

Hydroxyurea treatment consistently lowers WBC and ANC without anemia improvement during a 17-week period. At 50 mg/kg, hydroxyurea creates a decreased white blood cell count, zero neutrophil count, and no improvement in anemia when compared to sickle cell mice receiving a vehicle treatment.

Cell Assay

The same patients' erythroid cells from their peripheral blood are treated with hydroxyurea in vitro one year after they stopped taking it orally for two years, starting at a dose of 5 mg/kg/day for five days a week and increasing to a maximum of 10 mg/kg/day. Thirteen β-Thal/HbE patients receive this treatment.Cells are treated in primary culture for 96 hours with 30 μM hydroxyurea.

Animal Protocol

Mice: SCD mice are given hydroxyurea at doses of 25 mg/kg, 50 mg/kg, and 100 mg/kg, or vehicle, five days a week, to investigate whether hydroxyurea would improve anemia and/or prevent or lessen the development of organ damage in the absence of HbF induction.

References

[1]. Clin Infect Dis . 2000 Jun:30 Suppl 2:S193-7.

[2]. Clin Infect Dis . 2000 Jun:30 Suppl 2:S143-50.

[3]. Exp Hematol . 2005 Dec;33(12):1486-92.

[4]. Gene Ther . 2002 Aug;9(15):1023-30.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

CH4N2O2

Molecular Weight

76.05

Exact Mass

76.03

Elemental Analysis

C, 15.79; H, 5.30; N, 36.83; O, 42.07

CAS #

127-07-1

Related CAS #

127-07-1

Appearance

Solid powder

SMILES

C(=O)(N)NO

InChi Key

VSNHCAURESNICA-UHFFFAOYSA-N

InChi Code

InChI=1S/CH4N2O2/c2-1(4)3-5/h5H,(H3,2,3,4)

Chemical Name

hydroxyurea

Synonyms

NCI-c04831; NSC-32065; NCI c04831; NSC 32065; NCIc04831; NSC32065; Biosupressin; Carbamoyl oxime; Droxia; Hydroxycarbamide

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 15~50 mg/mL (197.2~657.5 mM)

Water: ~15 mg/mL (~197.2 mM)

Ethanol: <1 mg/mL

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	13.1492 mL	65.7462 mL	131.4924 mL
	5 mM	2.6298 mL	13.1492 mL	26.2985 mL
	10 mM	1.3149 mL	6.5746 mL	13.1492 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01966731	Active Recruiting	Drug: Hydroxyurea	Sickle Cell Disease	Children's Hospital Medical Center, Cincinnati	June 2014	Phase 1 Phase 2
NCT04750707	Active Recruiting	Drug: Hydroxyurea	Sickle Cell Anemia in Children	Global Health Uganda LTD	March 9, 2021	Phase 3
NCT04691323	Active Recruiting	Other: HU-Go app	Sickle Cell Disease Sickle B+ Thalassemia	Ann & Robert H Lurie Children's Hospital of Chicago	March 2, 2021	Not Applicable
NCT05485948	Active Recruiting	Drug: Ropeginterferon alfa-2b	Polycythemia Vera	PharmaEssentia	October 8, 2021	Phase 2
NCT02493530	Active Recruiting	Drug: TGR-1202 Drug: ruxolitinib	Myelofibrosis Polycythemia Vera	Vanderbilt-Ingram Cancer Center	July 2015	Phase 1

Biological Data

Effect of hydroxyurea treatment on fractional fetal hemoglobin (HbF) (high-performance liquid chromatography analysis), fold induction of ^Gγ:^Aγ-globin mRNA (real-time one-step quantitative competitive reverse transcriptase-polymerase chain reaction), and ^Gγ:^Aγ-globin ratio (Triton X-100 acid urea polyacrylamide gel electrophoresis) in β-thalassemia/hemoglobin E (β-thal/HbE) patients in vitro vs in vivo. Exp Hematol . 2005 Dec;33(12):1486-92.