| 产品描述： | Etrumadenant (AB928, A2aR/A2bR antagonist-1)是一种新型的 A2aR/A2bR 的双重活性拮抗剂，对于A2aR和A2bR的Kd值分别为1.4 nM和2 nM |
| 靶点： |
A2AR(Cell-free assay):1.4 nM(Kd); A2bR(Cell-free assay):2 nM(Kd) |
| 体外研究： |
Consistent with the ability of adenosine to suppress immune function, AB928 inhibits the ability of adenosine to suppress CD4 or CD8 T cell activation |
| 体内研究： |
Established AT-3-OVA tumors treated with AB928 alone has a small but significant decrease in their growth rate. Concurrent treatment with AB928 and chemotherapy results in significantly reduced tumor growth rates, when compared to chemotherapy alone |
| 细胞实验： |
Cell lines: CD4+ T cells, CD8+ T cells Concentrations: 1 nM, 3 nM, 10 nM, 30 nM Incubation Time: -- Method: CD4+ or CD8+ T cells are isolated from PBMC using RosetteSep separation and are stimulated with CD2/CD3/CD28 microbeads +/- adenosine/EHNA +/- AB928. Human CD14+ cells are differentiated into moDC for 6 days in IL-4/GM-CSF +/- adenosine/EHNA, +/- AB928. Adenosine is present during moDC activation via IFN-y or LPS. Cells are washed in excess buffer, to remove residual adenosine, prior to setting up the mixed leukocyte reaction (MLR). Supernatants are collected 4 days after initiation of the moDC/CD4 co-culture. |
| 动物实验： |
Animal Models: female C57BL/6 mice Dosages: 100 mg/kg Administration: Oral gavage |
| 参考文献： |
1. Lisa Seitz, et al. Safety, tolerability, and pharmacology of AB928, a novel dual adenosine receptor antagonist, in a randomized, phase 1 study in healthy volunteers. Invest New Drugs. 2019 Aug;37(4):711-721. 2. Walters MJ, et al. Abstract 5556: Combining adenosine receptor inhibition with AB928 and chemotherapy results in greater immune activation and tumor control. Cancer Res 2018;78(13 Suppl):Abstract nr 5556. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.345 ml |
11.724 ml |
23.448 ml |
| 5 mM |
0.469 ml |
2.345 ml |
4.69 ml |
| 10 mM |
0.234 ml |
1.172 ml |
2.345 ml |
| 50 mM |
0.047 ml |
0.234 ml |
0.469 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京