Brequinar (Synonyms: 布喹那; DUP785; NSC 368390)

目录号: HY-108325 纯度: 99.75%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Brequinar (DUP785) 是一种有效的 dihydroorotate dehydrogenase (DHODH) 抑制剂，对人的 IC₅₀ 值为 5.2 nM，也是一种广谱的抗病毒剂，同时具有抗 SARS2 的活性。

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Brequinar Chemical Structure

CAS No. : 96187-53-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥770	In-stock
5 mg	￥700	In-stock
10 mg	￥1020	In-stock
50 mg	￥2090	In-stock
100 mg	￥3150	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Brequinar:

Brequinar sodium 询价

MCE 顾客使用本产品发表的 17 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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.

细胞效力
(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]
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]
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]
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]
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	> 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]
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]
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]
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]
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]

体外研究
(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].

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

体内研究
(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].

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

Clinical Trial

分子量

375.37

Formula

C₂₃H₁₅F₂NO₂

CAS 号

96187-53-0

性状

固体

颜色

White to off-white

中文名称

布喹那

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (66.60 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (5.54 mM); 悬浊液; 超声加热助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.54 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 5 mg/mL (13.32 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (26.64 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.75%

选择批次：

Data Sheet (631 KB) SDS (393 KB)

COA (288 KB) HNMR (283 KB) LCMS (95 KB)

产品使用指南 (1538 KB)

参考文献

[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.
参考文献	[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]

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完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

Help & FAQs

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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Brequinar (Synonyms: 布喹那; DUP785; NSC 368390)

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