Brequinar (Synonyms: DUP785; NSC 368390)

Name: Brequinar
Brand: MedChemExpress
SKU: HY-108325
Rating: 5.0 (28 reviews)

Cat. No.: HY-108325 Purity: 99.94%: Data Sheet
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Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC₅₀ of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

For research use only. We do not sell to patients.

CAS No. : 96187-53-0

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 28 publication(s) in Google Scholar

Other Forms of Brequinar:

28 Publications Citing Use of MCE Brequinar

Microbiological Assay

In Vivo Efficacy Study

Histological Imaging/Staining

Bio/Physico-chemical Assay

: Brequinar purchased from MedChemExpress. Usage Cited in: Nature. 2024 Feb;626(7998):411-418. [Abstract]; Mitochondrial lipid peroxidation assessment of HT1080 treated with RSL3 (0.5 μM) and BQR (Brequinar 200 μM) for 2 h after pretreatment of 7-DHC (25 μM) and Fer-1 for 24 h.

: Brequinar purchased from MedChemExpress. Usage Cited in: Nature. 2022 Apr;604(7904):134-140. [Abstract]; Anti-SARS2 activity of Brequinar (0-10 μM, 1 h pretreatment and infected for 40-48 h).

: Brequinar purchased from MedChemExpress. Usage Cited in: Nature. 2022 Apr;604(7904):134-140. [Abstract]; Lungs analyzed for viral titer by plaque assay. Wild type Balb/C mice were treated with Brequinar (IP) and/or molnupiravir (EIDD-2801) (PO) daily at the indicated concentrations starting 24 h after infection. Mice (N = 5 mice per group) were intranasally inoculated with 1×10^5 PFU/mouse of SARS-CoV-2/B.1.351.

: Brequinar purchased from MedChemExpress. Usage Cited in: Nature. 2022 Apr;604(7904):134-140. [Abstract]; Lungs quantified for interstitial inflammation. Wild type Balb/C mice were treated with Brequinar (IP) and/or molnupiravir (EIDD-2801) (PO) daily at the indicated concentrations starting 24 h after infection. Mice (N = 5 mice per group) were intranasally inoculated with 1×10^5 PFU/mouse of SARS-CoV-2/B.1.351.

: Brequinar purchased from MedChemExpress. Usage Cited in: Nature. 2022 Apr;604(7904):134-140. [Abstract]; Lungs fixed in 4% PFA for H&E staining (Scale bar = 200 μm). Wild type Balb/C mice were treated with Brequinar (IP) and/or molnupiravir (EIDD-2801) (PO) daily at the indicated concentrations starting 24 h after infection. Mice (N = 5 mice per group) were intranasally inoculated with 1×10^5 PFU/mouse of SARS-CoV-2/B.1.351.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.59 μM Compound: BRQ	Antiproliferative activity against human A375 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
A549	IC₅₀	4.1 μM Compound: BRQ	Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
Bone marrow cell	EC₅₀	0.51 μM Compound: Brequinar	Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry	[PMID: 27994748]
Caco-2	CC₅₀	231.3 μM Compound: 45	Cytotoxicity against human Caco-2 cells assessed as reduction in cell growth measured fpr 48 hrs by MTT assay Cytotoxicity against human Caco-2 cells assessed as reduction in cell growth measured fpr 48 hrs by MTT assay	[PMID: 38160620]
HCT-116	IC₅₀	0.679 μM Compound: 1	Antiproliferative activity against human HCT116 cells over-expressing DHODH after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells over-expressing DHODH after 72 hrs by MTT assay	[PMID: 29727569]
HCT-116	IC₅₀	4.12 μM Compound: BRQ	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
HL-60	IC₅₀	0.544 μM Compound: 1	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 29727569]
HT-1080	IC₅₀	0.21 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 33007554]
HT-1080	IC₅₀	17 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay	[PMID: 33007554]
HT-29	IC₅₀	0.59 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 33007554]
HT-29	IC₅₀	24 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay	[PMID: 33007554]
HeLa	IC₅₀	> 10 μM Compound: BRQ	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
Jurkat	IC₅₀	0.2 μM Compound: 26	Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay	[PMID: 26079043]
Jurkat	IC₅₀	0.91 μM Compound: Brequinar	Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay	[PMID: 29939742]
Jurkat	IC₅₀	0.93 μM Compound: BQN	Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method	[PMID: 28235702]
Jurkat	IC₅₀	94.17 μM Compound: Brequinar	Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay	[PMID: 29939742]
K562	IC₅₀	0.54 μM Compound: BRQ	Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
M21	IC₅₀	0.57 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 33007554]
M21	IC₅₀	25 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay Antiproliferative activity against human M21 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay	[PMID: 33007554]
MCF7	IC₅₀	25 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs in presence of uridine by SRB assay	[PMID: 33007554]
MCF7	IC₅₀	5.1 μM Compound: DUP-785; NSC 368390	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 33007554]
MCF7	IC₅₀	> 10 μM Compound: BRQ	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
MDA-MB-231	IC₅₀	0.31 μM Compound: Brequinar	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 34516133]
MDA-MB-468	IC₅₀	0.082 μM Compound: Brequinar	Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent assay	[PMID: 34516133]
MDCK	EC₅₀	0.3 μM Compound: brequinar	Antiviral activity against VSV infected in MDCK cells assessed as inhibition of VSV replication after 48 hrs by plaque assay Antiviral activity against VSV infected in MDCK cells assessed as inhibition of VSV replication after 48 hrs by plaque assay	[PMID: 23930152]
MDCK	EC₅₀	460 nM Compound: brequinar	Antiviral activity against influenza A virus A/WSN/33 (H0N1) infected in MDCK cells after 48 hrs by plaque assay Antiviral activity against influenza A virus A/WSN/33 (H0N1) infected in MDCK cells after 48 hrs by plaque assay	[PMID: 23930152]
MIA PaCa-2	IC₅₀	1.69 μM Compound: 1	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay	[PMID: 29727569]
MOLM-13	IC₅₀	60 nM Compound: 1; BRQ	Antiproliferative activity against human MOLM-13 cells Antiproliferative activity against human MOLM-13 cells	[PMID: 33007394]
NAMALVA	IC₅₀	> 10 μM Compound: BRQ	Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
OCI-AML2	IC₅₀	200 nM Compound: 40; CS2	Antiproliferative activity against human OCI-AML2 cells assessed as reduction in cell viability Antiproliferative activity against human OCI-AML2 cells assessed as reduction in cell viability	[PMID: 38805939]
PBMC	IC₅₀	3.74 μM Compound: Brequinar	Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by Hoechst 33258 dye-based fluorescence assay	[PMID: 29939742]
PBMC	IC₅₀	4.3 μM Compound: BQN	Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by BrdU incorporation assay Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs by BrdU incorporation assay	[PMID: 28235702]
PBMC	IC₅₀	59.64 μM Compound: Brequinar	Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay Immunosuppressive activity against human PBMC assessed as inhibition of PHA-stimulated cell proliferation preincubated for 2 hrs followed by PHA stimulation for 72 hrs in presence of exogenous uridine by Hoechst 33258 dye-based fluorescence assay	[PMID: 29939742]
Raji	IC₅₀	2.29 μM Compound: BRQ	Antiproliferative activity against human Raji cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 32496056]
THP-1	EC₅₀	0.094 μM Compound: Brequinar	Induction of human THP1 cell differentiation after 4 days by flow cytometry Induction of human THP1 cell differentiation after 4 days by flow cytometry	[PMID: 27994748]
THP-1	EC₅₀	0.2486 μM Compound: Brequinar	Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis Induction of cell differentiation in human THP-1 cells assessed as CD14 expression after 3 days by flow cytometric analysis	[PMID: 33844533]
THP-1	EC₅₀	0.264 μM Compound: Brequinar	Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry Induction of apoptosis in human THP-1 cells after 3 days by Annexin-V-FITC staining based flow cytometry	[PMID: 33844533]
THP-1	EC₅₀	249 nM Compound: Brequinar	Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis Induction of cell differentiation in human THP-1 cells measured for 2 days by flow cytometric analysis	[PMID: 36162075]
THP-1	EC₅₀	264 nM Compound: Brequinar	Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis Induction of apoptosis in human THP-1 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis	[PMID: 36162075]
U-937	EC₅₀	0.044 μM Compound: Brequinar	Induction of human U937 cell differentiation after 4 days by flow cytometry Induction of human U937 cell differentiation after 4 days by flow cytometry	[PMID: 27994748]
U-937	EC₅₀	0.1886 μM Compound: Brequinar	Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis	[PMID: 33844533]
U-937	EC₅₀	0.3222 μM Compound: Brequinar	Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry Induction of apoptosis in human U-937 cells after 3 days by Annexin-V-FITC staining based flow cytometry	[PMID: 33844533]
U-937	EC₅₀	214 nM Compound: Brequinar	Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis	[PMID: 36162075]
U-937	EC₅₀	262 nM Compound: Brequinar	Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis Induction of apoptosis in human U-937 cells measured after 3 days by Annexin-V-FITC staining based FACS analysis	[PMID: 36162075]

In Vitro

Brequinar reduces virus progeny production by >90%, with EC₅₀ of 17 nM. Brequinar (5 μM) also inhibits other orthopoxviruses, and blocks virus DNA replication. Brequinar does not affect virus early gene expression, but has a severe effect on the late stage of the virus cycle^[1]. Brequinar reduces the level of envelope protein production and the viral titer in a dose-dependent manner, with EC₅₀ of 78 nM in the CFI assay. Brequinar (5 μM) inhibits viral RNA synthesis. Brequinar has antiviral effect, but the effect is reversed by pyrimidine. Brequinar-resistant viruses can be selected in cell culture. Brequinar (5 μM) suppresses the luciferase activities from both the WT and NS5 mutant replicons^[2]. Brequinar sodium effectively prevents the increase in PyNTP levels with an IC₅₀ of 0.26 μM. Brequinar sodium effectively inhibits cell proliferation with an IC₅₀ of 0.26 μM. Brequinar sodium inhibits autophosphorylation of p56^lck with IC₅₀ of 70 μM; inhibition is 39, 41, and 60% for 25, 50, and 100 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p56^lck of the exogenous substrate, histone 2B, with an IC₅₀ of 70 μM; inhibition is 10, 43, 59, and 86% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium inhibits autophosphorylation of p59^fyn with an IC₅₀ of 105 μM; inhibition is 0, 17, 48, and 65% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p59^fyn of histone 2B with an IC₅₀ of 20 μM; inhibition is 26, 54, 79, 83, and 84% for 10, 25, 50, 100, and 200 μM Brequinar sodium, respectively^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Brequinar sodium-treated (10-20 mg/kg/day) mice has a 31% reduction in percentage of packed cell volume compared with untreated BALB/c mice. Brequinar sodium reduces UTP and CTP levels in bone marrow cells by 30 and 25%, respectively. Brequinar sodium (10-20 mg/kg/day) in combination with uridine (1000-2000 mg/kg/day) prevents anemia, and the hematocrits remain at levels (61-63%) comparable with those of untreated controls^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

375.37

Formula

C₂₃H₁₅F₂NO₂

CAS No.

96187-53-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)C(C2=CC=C(C3=CC=CC=C3F)C=C2)=NC4=CC=C(F)C=C14)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (66.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : < 1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6640 mL	13.3202 mL	26.6404 mL
5 mM	0.5328 mL	2.6640 mL	5.3281 mL
10 mM	0.2664 mL	1.3320 mL	2.6640 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (5.54 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (13.32 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (26.64 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (282 KB) SDS (396 KB)

COA (250 KB) HNMR (273 KB) RP-HPLC (262 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Schnellrath LC, et al. Potent antiviral activity of brequinar against the emerging Cantagalo virus in cell culture. Int J Antimicrob Agents. 2011 Nov;38(5):435-41. [Content Brief]

[2]. Qing M, et al. Characterization of dengue virus resistance to brequinar in cell culture. Antimicrob Agents Chemother. 2010 Sep;54(9):3686-95. [Content Brief]

[3]. Xu X, et al. In vitro and in vivo mechanisms of action of the antiproliferative and immunosuppressive agent, brequinar sodium. J Immunol. 1998 Jan 15;160(2):846-53. [Content Brief]

[4]. Zeping Zuo, et al. Bifunctional Naphtho[2,3-d][1,2,3]triazole-4,9-dione Compounds Exhibit Antitumor Effects In Vitro and In Vivo by Inhibiting Dihydroorotate Dehydrogenase and Inducing Reactive Oxygen Species Production. J Med Chem. 2020 Jun 4. [Content Brief]

[5]. David C Schultz, et al. Pyrimidine inhibitors synergize with nucleoside analogues to block SARS-CoV-2. Nature. 2022 Feb 7. [Content Brief]

Kinase Assay ^[3]	Immunoprecipitated p59^fyn or p56^lck from CTLL-4 cells or LSTRA cells (5×10⁶) is preincubated with various concentrations of BQR in the PTK buffer (50 mM HEPES (pH 7.4), 10 mM MgCl₂, and 10 mM MnCl₂) on ice for 10 min. Exogenous substrate, histone 2B (2 μg), is added and, after 10 min, the reaction is initiated by addition of 10 μCi [γ-³²P]ATP. After incubation at 20°C for 10 min, the reaction mixture is subjected to electrophoresis in a 12.5% SDS-polyacrylamide gel. Phosphorylation of the kinase and the exogenous substrate is analyzed by autoradiography. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	The neutral-red uptake assay is used to evaluate cell viability. BSC-40 cells are seeded in 96-well plates in the presence of concentrations of Brequinar ranging from 0.01 μM to 75 μM for 24 h. Control cells are incubated with 0.1% DMSO. Neutral red is methanol/acetic acid-extracted from cells and is quantitated at an absorbance of 490 nm (A490). All measurements expressed the average of four independent assays. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Brequinar is administered once daily by i.p. injection, while uridine is administered twice daily. Mice are bled through the orbital vein using a microhematocrit capillary tube, and the blood is centrifuged for 10 min at 550 × g. The percentage of packed cell volumes is determined with a microhematocrit capillary tube reader. All mice are killed 4 h after receiving their last dose of Brequinar or uridine. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Schnellrath LC, et al. Potent antiviral activity of brequinar against the emerging Cantagalo virus in cell culture. Int J Antimicrob Agents. 2011 Nov;38(5):435-41. [Content Brief] [2]. Qing M, et al. Characterization of dengue virus resistance to brequinar in cell culture. Antimicrob Agents Chemother. 2010 Sep;54(9):3686-95. [Content Brief] [3]. Xu X, et al. In vitro and in vivo mechanisms of action of the antiproliferative and immunosuppressive agent, brequinar sodium. J Immunol. 1998 Jan 15;160(2):846-53. [Content Brief] [4]. Zeping Zuo, et al. Bifunctional Naphtho[2,3-d][1,2,3]triazole-4,9-dione Compounds Exhibit Antitumor Effects In Vitro and In Vivo by Inhibiting Dihydroorotate Dehydrogenase and Inducing Reactive Oxygen Species Production. J Med Chem. 2020 Jun 4. [Content Brief] [5]. David C Schultz, et al. Pyrimidine inhibitors synergize with nucleoside analogues to block SARS-CoV-2. Nature. 2022 Feb 7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6640 mL	13.3202 mL	26.6404 mL	66.6010 mL
	5 mM	0.5328 mL	2.6640 mL	5.3281 mL	13.3202 mL
	10 mM	0.2664 mL	1.3320 mL	2.6640 mL	6.6601 mL
	15 mM	0.1776 mL	0.8880 mL	1.7760 mL	4.4401 mL
	20 mM	0.1332 mL	0.6660 mL	1.3320 mL	3.3300 mL
	25 mM	0.1066 mL	0.5328 mL	1.0656 mL	2.6640 mL
	30 mM	0.0888 mL	0.4440 mL	0.8880 mL	2.2200 mL
	40 mM	0.0666 mL	0.3330 mL	0.6660 mL	1.6650 mL
	50 mM	0.0533 mL	0.2664 mL	0.5328 mL	1.3320 mL
	60 mM	0.0444 mL	0.2220 mL	0.4440 mL	1.1100 mL

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Brequinar96187-53-0DUP785 NSC 368390DUP 785DUP-785NSC368390NSC 368390NSC-368390Dihydroorotate DehydrogenaseSARS-CoVVirus ProteaseDNA/RNA SynthesisDHODHSARS coronavirusInhibitorinhibitorinhibit

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Brequinar (Synonyms: DUP785; NSC 368390)

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