Brequinar
别名: DUP785, NSC 368390 中文名称：布喹那
Brequinar是二氢乳清酸脱氢酶DHODH抑制剂，在体外IC50约为20 nM。
Brequinar Chemical Structure
CAS: 96187-53-0
客户使用Selleck的发表文献8篇
产品质控
相关信号通路图
Dehydrogenase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HCT116 | Cytostatic activity assay | 10 uM | 24 hrs | Cytostatic activity against human HCT116 cells assessed as reduction in colony forming at 10 uM after 24 hrs by crystal violet staining based assay | 29727569 |
| HCT116 | Cytostatic activity assay | 10 uM | 7 days | Cytostatic activity against human HCT116 cells assessed as reduction in colony forming at 10 uM after 7 days by crystal violet staining based assay | 29727569 |
| U937 | Antiproliferative assay | 0.01 to 10 uM | 3 days | Antiproliferative activity against CFSE-labeled human U937 cells at 0.01 to 10 uM after 3 days by propidium iodide staining-based flow cytometry | 29939742 |
| THP1 | Antiproliferative assay | 0.01 to 10 uM | 3 days | Antiproliferative activity against CFSE-labeled human THP1 cells at 0.01 to 10 uM after 3 days by propidium iodide staining-based flow cytometry | 29939742 |
| U937 | Function assay | 0.1 to 10 uM | up to 4 days | Induction of myeloid differentiation in human U937 cells assessed as increase in CD11b expression level at 0.1 to 10 uM up to 4 days by propidium iodide staining-based flow cytometry | 29939742 |
| THP1 | Function assay | 0.1 to 10 uM | up to 5 days | Induction of myeloid differentiation in human THP1 cells assessed as increase in CD11b expression level at 0.1 to 10 uM up to 5 days by propidium iodide staining-based flow cytometry | 29939742 |
| THP1 | Function assay | 0.1 to 10 uM | up to 5 days | Induction of myeloid differentiation in human THP1 cells assessed as increase in CD14 expression level at 0.1 to 10 uM up to 5 days by propidium iodide staining-based flow cytometry | 29939742 |
| Jurkat | Antiproliferative assay | 72 hrs | Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay, IC50=0.2μM | 26079043 | |
| MDCK | Antiviral assay | 48 hrs | Antiviral activity against VSV infected in MDCK cells assessed as inhibition of VSV replication after 48 hrs by plaque assay, EC50=0.3μM | 23930152 | |
| MDCK | Antiviral assay | 48 hrs | Antiviral activity against influenza A virus A/WSN/33 (H0N1) infected in MDCK cells after 48 hrs by plaque assay, EC50=0.46μM | 23930152 | |
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.544μM | 29727569 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells over-expressing DHODH after 72 hrs by MTT assay, IC50=0.679μM | 29727569 | |
| Jurkat T | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay, IC50=0.91μM | 29939742 | |
| Jurkat T | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method, IC50=0.93μM | 28235702 | |
| MIAPaCa2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay, IC50=1.69μM | 29727569 | |
| Jurkat T | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Jurkat T cells assessed as compound concentration required to induce up to 30% cell death after 72 hrs by Hoechst 33258 dye based fluorometric method, Activity=45μM | 28235702 | |
| Jurkat T | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Jurkat T cells assessed as compound concentration required to induce =>30% cell death after 72 hrs by CellTox green assay, Activity=48.2μM | 29939742 | |
| HCT116 | Growth inhibition assay | 72 hrs | Growth inhibition of human HCT116 cells over-expressing DHODH at 2 times antiproliferative IC50 after 72 hrs in absence of uridine by MTT assay | 29727569 | |
| insect cells | Function assay | Inhibition of human recombinant DHODH expressed in baculovirus infected insect cells using dihydroorotate as substrate in presence of quinone by dichlorophenol-indophenol dye based assay, IC50=0.01μM | 27994748 | ||
| A549 | Antiviral assay | Antiviral activity against Yellow fever virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM | 31557612 | ||
| A549 | Antiviral assay | Antiviral activity against West Nile virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM | 31557612 | ||
| A549 | Antiviral assay | Antiviral activity against Dengue virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM | 31557612 | ||
| A549 | Antiviral assay | Antiviral activity against Western equine encephalomyelitis virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM | 31557612 | ||
| A549 | Antiviral assay | Antiviral activity against Vesicular stomatitis virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM | 31557612 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Brequinar是二氢乳清酸脱氢酶DHODH抑制剂，在体外IC50约为20 nM。 | ||
|---|---|---|---|
| 靶点 |
|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03760666 | Terminated | Acute Myeloid Leukemia |
Clear Creek Bio Inc. |
December 20 2018 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 375.37 | 分子式 | C23H15F2NO2 |
| CAS号 | 96187-53-0 | SDF | -- |
| Smiles | CC1=C(C2=C(C=CC(=C2)F)N=C1C3=CC=C(C=C3)C4=CC=CC=C4F)C(=O)O | ||
| 储存条件(自收到货起) | 3年 -20°C 粉状 | ||
|
体外溶解度 |
DMSO : 37 mg/mL ( (98.56 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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