| Identification | Back Directory | [Name]
(R)-N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine | [CAS]
2247953-39-3 | [Synonyms]
AHR antagonist 5
(R)-N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine | [Molecular Formula]
C25H25ClFN7 | [MDL Number]
MFCD34470337 | [MOL File]
2247953-39-3.mol | [Molecular Weight]
477.97 |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[1]. Alfredo C. Castro, et al. Indole ahr inhibitors and uses thereof. WO2018195397A2. |
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