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Brequinar
別名: DUP785, NSC 368390 中文名稱：布喹那
Brequinar是二氫乳清酸脫氫酶DHODH抑制劑，在體外IC50約為20 nM。
Brequinar Chemical Structure
CAS: 96187-53-0
產(chǎn)品質(zhì)控
批次：
純度：
99.93%
99.93
Brequinar相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Brequinar是二氫乳清酸脫氫酶DHODH抑制劑，在體外IC50約為20 nM。 | ||
|---|---|---|---|
| 靶點 |
|
| 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 |
化學信息&溶解度
| 分子量 | 375.37 | 分子式 | C23H15F2NO2 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | 3年 -20°C 粉狀 | ||
|
體外溶解度 |
DMSO : 37 mg/mL ( (98.56 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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