| 产品描述： | AhR抑制剂;AhR Inhibitors;;InformationBAY-218 BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands.TargetsAhRIn vitroMechanistically, BAY-218 inhibits AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. BAY-218 rescues TNFα production from kynurenic acid(KA)-suppressed LPS-treated primary human monocytes.In vivoBAY-218 enhances anti-tumoral immune responses and reduced tumor growth in the syngeneic mouse tumor models CT26 and B16-OVA. Furthermore, BAY-218 enhances therapeutic efficacy of an anti-PD-L1 antibody in the CT26 model. |
| 靶点： |
IC50: 39.9 nM (AHR in human cell line) |
| 体内研究： |
BAY-218 (example 23) (口服 30 mg/kg；bid) 与 aPD-L1 联用具有良好的抗肿瘤作用。 |
| 参考文献： |
1. Norbert Schmees, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides. WO2017202816A1. |
| 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 |
2.489 ml |
12.443 ml |
24.887 ml |
| 5 mM |
0.498 ml |
2.489 ml |
4.977 ml |
| 10 mM |
0.249 ml |
1.244 ml |
2.489 ml |
| 50 mM |
0.05 ml |
0.249 ml |
0.498 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)
