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Chemical Structure| 96201-88-6 Chemical Structure| 96201-88-6

Structure of Brequinar Sodium
CAS No.: 96201-88-6

Chemical Structure| 96201-88-6

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Brequinar sodium is a potent inhibitor of the mitochondrial DHODH, a rate-limiting enzyme in the pyrimidine de novo nucleotide synthesis.

Synonyms: DuP785 sodium; NSC 368390 sodium; NSC 368390

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Product Details of Brequinar Sodium

CAS No. :96201-88-6
Formula : C23H14F2NNaO2
M.W : 397.35
SMILES Code : O=C(C1=C(C)C(C2=CC=C(C3=CC=CC=C3F)C=C2)=NC4=CC=C(F)C=C14)[O-].[Na+]
Synonyms :
DuP785 sodium; NSC 368390 sodium; NSC 368390
MDL No. :MFCD22648381

Safety of Brequinar Sodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
GMPs 1 μM BRQ treatment reduced the capacity of GMPs to develop into immune-suppressive MDSCs PMC9711879
BM cells 1 μM 96 h BRQ treatment reduced the ability of MDSCs to inhibit CD4+ and CD8+ T cell proliferation PMC9711879
U937 cells 0.5 μM 72 h To test the effects of brequinar on cell cycle and expression of differentiation markers. PMC6802504
THP-1 cells 0.5 μM 72 h To test the effects of brequinar in other monocytic cell lines. The results showed that brequinar caused S-phase arrest and increased the expression of differentiation markers, which could be reversed by the addition of uridine PMC6802504
MOLM-14 cells 0.5 μM 72 h To test the effects of brequinar in other monocytic cell lines. The results showed that brequinar caused S-phase arrest and increased the expression of differentiation markers, which could be reversed by the addition of uridine PMC6802504
HL-60 cells 0.5 μM 72 h To test the effects of brequinar in other monocytic cell lines. The results showed that brequinar caused S-phase arrest and increased the expression of differentiation markers, which could be reversed by the addition of uridine PMC6802504
A549/ACE2 cells 1.25–5.0 μM 48 h Evaluate the antiviral activity of BRQ combined with DPY against SARS-CoV-2 Delta variant. Results showed enhanced antiviral activity. PMC9420051
A549/ACE2 cells 0.0781–5 μM 48 h Evaluate the antiviral activity of BRQ combined with DPY against SARS-CoV-2 Beta variant. Results showed synergistic antiviral activity with significantly reduced EC50 values. PMC9420051
HEK-293T-hACE2 cells 1 μM 4 h Evaluate the effect of BRQ combined with DPY on intracellular pyrimidine nucleotide (CTP and UTP) concentrations in the presence of high exogenous uridine (20 μM). Results showed that the combination significantly reduced CTP and UTP concentrations even in the presence of high exogenous uridine. PMC9420051
A549/ACE2 cells 1 μM 8 h Evaluate the effect of BRQ combined with DPY on intracellular pyrimidine nucleotide (CTP and UTP) concentrations. Results showed that the combination significantly reduced CTP and UTP concentrations at 2 h, 4 h, and 8 h, with a more pronounced effect than BRQ alone. PMC9420051
IPEC-J2 cells 500 nM 24 h Inhibited CSFV replication more effectively in IPEC-J2 cells compared to PK-15 and BHK cells. PMC11237749
murine spleen cells 0.001 μg/ml to 10 μg/ml 72 h BQR caused dose-dependent inhibition of strong proliferative responses induced by Con A or PMA + ionomycin, with residual proliferation persisting even at the highest BQR concentrations. No impairment of low-concentration Con A, anti-CD3, or anti-Igs responses was observed. PMC2978649

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice 4T1 and E0771.ML-1 tumor models Intraperitoneal injection 10 mg/kg Daily administration, starting when tumors became measurable BRQ alone had minimal effects on primary tumor growth but significantly inhibited tumor growth and lung metastasis when combined with anti-PD-1 antibody PMC9711879

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.17mL

5.03mL

2.52mL

References

 

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