AHR antagonist 5 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 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。
货号:ajcx37298
CAS:2247953-39-3
分子式:C25H27Cl3FN7
分子量：550.89
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of< 0.5 µμ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1[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].

[1]. Alfredo C. Castro, et al. Indole ahr inhibitors and uses thereof. WO2018195397A2.