受注:045-509-1970 |
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Synonyms | DUP785, NSC 368390 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C23H15F2NO2 |
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分子量 | 375.37 | CAS No. | 96187-53-0 | |
Solubility (25°C)* | 体外 | DMSO | 37 mg/mL (98.56 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. |
製品説明 | Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro. |
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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] |
細胞アッセイ | 細胞株 | splenic T cells isolated from BALB/c mice |
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濃度 | 0.26, 1.3, 2.6 μM | |
反応時間 | 40-66 h | |
実験の流れ | 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. |
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動物実験 | 動物モデル | BALB/c mice |
投薬量 | 10-20 mg/kg/day | |
投与方法 | i.p. |
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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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。