Brequinar

Catalog No.S6626 Batch:S662604

Technical Data

Formula	C₂₃H₁₅F₂NO₂
Molecular Weight	375.37	CAS No.	96187-53-0
Solubility (25°C)*	In vitro	DMSO	9 mg/mL (23.97 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.

Targets

DHODH ^[1]

20 nM

In vitro

Brequinar sodium (BQR) reduces of PyN levels in Con A-stimulated T cells and inhibition of cell proliferation at low concentrations, which can be reversed by uridine. However, uridine is unable to reverse the effects of high concentrations of BQR. BQR possesses the ability of inhibiting tyrosine phosphorylation.^[2]

In vivo

Brequinar sodium (BQR) induces anemia through inhibition of DHO-DHase activity and de novo pyrimidine synthesis in vivo. Coadministration of BQR with uridine prevents anemia.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines splenic T cells isolated from BALB/c mice Concentrations 0.26, 1.3, 2.6 μM Incubation Time 40-66 h Method Lymphocytes are isolated from BALB/c spleen by centrifugation through a Ficol gradient and are depleted of macrophages and B cells by adherence to goat anti-mouse IgG-coated plates. The nonadherent cells are harvested and cultured at 4 to 5× 10⁵/ml in RPMI 1640 supplemented with 10% FBS. Stimulation is performed with 5 μg/ml Con A in the presence of indicated concentrations of Brequinar or uridine. After 40 to 66 h, the cells are harvested and the levels of cell proliferation or purine NTP and PyNTP are quantified.

Cell Assay:^{^[2]}

Cell lines
splenic T cells isolated from BALB/c mice
Concentrations
0.26, 1.3, 2.6 μM
Incubation Time
40-66 h
Method
Lymphocytes are isolated from BALB/c spleen by centrifugation through a Ficol gradient and are depleted of macrophages and B cells by adherence to goat anti-mouse IgG-coated plates. The nonadherent cells are harvested and cultured at 4 to 5× 10⁵/ml in RPMI 1640 supplemented with 10% FBS. Stimulation is performed with 5 μg/ml Con A in the presence of indicated concentrations of Brequinar or uridine. After 40 to 66 h, the cells are harvested and the levels of cell proliferation or purine NTP and PyNTP are quantified.

References

Selleck's Brequinar has been cited by 8 publications

SIRT4 loss reprograms intestinal nucleotide metabolism to support proliferation following perturbation of homeostasis [ Cell Rep, 2024, 43(4):113975]	PubMed: 38507411
Gut microbiota-mediated nucleotide synthesis attenuates the response to neoadjuvant chemoradiotherapy in rectal cancer [ Cancer Cell, 2023, 41(1):124-138.e6]	PubMed: 36563680
Synchronous Disintegration of Ferroptosis Defense Axis via Engineered Exosome-Conjugated Magnetic Nanoparticles for Glioblastoma Therapy [ Adv Sci (Weinh), 2022, e2105451]	PubMed: 35508804
EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer [ Cell Rep, 2022, 41(11):111827]	PubMed: 36516759
Brequinar and dipyridamole in combination exhibits synergistic antiviral activity against SARS-CoV-2 in vitro: Rationale for a host-acting antiviral treatment strategy for COVID-19 [ Antiviral Res, 2022, 206:105403]	PubMed: 36041646
Inhibitors of dihydroorotate dehydrogenase cooperate with molnupiravir and N4-hydroxycytidine to suppress SARS-CoV-2 replication [ iScience, 2022, 25(5):104293]	PubMed: 35492218
Metabolic inhibitor screening identifies dihydrofolate reductase as an inducer of the tumor immune escape mediator CD24 [ Immunomedicine, 2022, 2(2)e1041]	PubMed: 36816458
N4-hydroxycytidine and inhibitors of dihydroorotate dehydrogenase synergistically suppress SARS-CoV-2 replication [ bioRxiv, 2021, 10.1101/2021.06.28.450163]	PubMed: N/A

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SHIPPING AND STORAGE
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