AHR antagonist 5 |
| カタログ番号GC64275 |
特許ＷＯ２０１８１９５３９７の実施例３９から抽出された強力で経口的に活性なアリール炭化水素受容体（ＡＨＲ）アンタゴニストであるＡＨＲアンタゴニスト５は、<０．５μＭのＩＣ５０を有する。 AHR アンタゴニスト 5 は、チェックポイント阻害剤の抗 PD-1 と組み合わせて、腫瘍の増殖を大幅に阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2247953-39-3
Sample solution is provided at 25 µL, 10mM.
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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.
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