AHR antagonist 5 hemimaleate

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AHR antagonist 5 hemimaleate 

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

AHR antagonist 5 hemimaleate Chemical Structure

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生物活性

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

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

499.55

Formula

C29H28FN7O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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

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