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Submit ReviewBrequinar sodium
说明： Potent and selective DHODH inhibitor
别名： BRQ,DuP 785,NSC 368390
化学名： 6-Fluoro-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium
纯度： ≥99% (HPLC)
生物活性 for Brequinar sodium
Brequinar sodium is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor (IC50 = ~20 nM). Causes depletion of pyrimidine nucleotides. Exhibits minimal inhibition against a panel of >400 kinases. Triggers differentiation of AML cell lines (ED50 = ~ 1 μM. Note uridine concentration effects ED50 value). Causes differentiation and depletion of leukemia-initiating cells in vivo. Antimetabolite.
化合物库 for Brequinar sodium
Brequinar sodium is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Brequinar sodium
| 分子量 | 397.35 |
| 公式 | C23H14F2NO2Na |
| 储存 | Store at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 96201-88-6 |
| PubChem ID | 23663964 |
| InChI Key | PZOHOALJQOFNTB-UHFFFAOYSA-M |
| Smiles | CC1=C(C2=CC(F)=CC=C2N=C1C3=CC=C(C4=C(C=CC=C4)F)C=C3)C(O[Na])=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Brequinar sodium
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 39.73 | 100 | |
| DMSO | 39.73 | 100 |
制备储备液 for Brequinar sodium
以下数据基于产品分子量 397.35。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.52 mL | 12.58 mL | 25.17 mL |
| 5 mM | 0.5 mL | 2.52 mL | 5.03 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.52 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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产品说明书 for Brequinar sodium
参考文献 for Brequinar sodium
参考文献是支持产品生物活性的出版物。
Arteaga (1989) Phase I clinical and pharmacokinetic trial of Brequinar sodium (DuP 785; NSC 368390). Cancer Res. 49 4648 PMID: 2743343
Sykes et al (2016) Inhibition of dihydroorotate dehydrogenase overcomes differentiation blockade in acute myeloid leukemia. Cell 167 171 PMID: 27641501
Peters et al (1987) Inhibition of pyrimidine de novo synthesis by DUP-785 (NSC 368390). Invest.New Drugs 5 235 PMID: 2822596
If you know of a relevant reference for Brequinar sodium, please let us know.
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关键词: Brequinar sodium, Brequinar sodium supplier, NSC368390, DuP785, BRQ, Biphenquinate, Brequinar, potent, selective, DHODH, inhibitors, inhibits, dihydroorotate, dehydrogenase, AML, acute, myeloid, leukemia, DuP, 785, NSC, 368390, Dihyroorotate, Dehydrogenase, DNA,, RNA, and, Protein, Synthesis, 6196, Tocris Bioscience
3 篇 Brequinar sodium 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Brequinar sodium 的部分引用包括：
Jessica A et al (2020) Inhibition of the de novo pyrimidine biosynthesis pathway limits ribosomal RNA transcription causing nucleolar stress in glioblastoma cells. PLoS Genet 16 e1009117 PMID: 33201894
Sonia et al (2021) DHODH inhibition modulates glucose metabolism and circulating GDF15, and improves metabolic balance. iScience 24 102494 PMID: 34113829
Juan et al (2022) Proof-of-principle studies on a strategy to enhance nucleotide imbalance specifically in cancer cells. Cell Death Discov 8 464 PMID: 36424385
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