AhR antagonist 5 hemimaleate 是有效的，具有口服活性的芳香烃受体(AhR)拮抗剂，IC50为< 0.5 μM。AhR antagonist 5 hemimaleate 联合检测点抑制剂 anti-PD-1 对肿瘤生长有抑制作用，详细信息请参见专利 WO2018195397，example 39。

AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC 50 of< 0.5 μΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39) [1].

Tumor growth inhibition is statistically significant with AHR antagonist 5 as single. AHR antagonist 5 (10 mg/kg; p.o.; every day for 3 weeks) combination with anti-PD-1 significantly inhibited tumor growth inhibition compared to the anti-PD-1 alone [1].

C29H28FN7O4

499.55

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years