AHR antagonist 5

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

AHR antagonist 5 

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。

AHR antagonist 5

AHR antagonist 5 Chemical Structure

CAS No. : 2247953-39-3

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生物活性

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].

体内研究
(In Vivo)

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.

Animal Model: Balb/c Mice (Mouse Colorectal Cancer Model CT26)[1]
Dosage: 10 mg/kg (combination with anti-PD-1)
Administration: P.o.; every day for 3 weeks
Result: Significantly inhibited tumor growth inhibition.

分子量

550.89

Formula

C25H27Cl3FN7

CAS 号

2247953-39-3

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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