| 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 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [form ]
Solid | [color ]
Yellow to orange | [InChIKey]
BCXFADDZDWTXMZ-VOPAOICTNA-N | [SMILES]
N([C@@H]1CCC2NC3=CC=CC=C3C=2C1)C1=NC(C2=CN=CC(F)=C2)=NC2=C(C(C)C)C=NN12.Cl |&1:1,r| |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | [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]. | 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.
|
| [References]
[1]. Alfredo C. Castro, et al. Indole ahr inhibitors and uses thereof. WO2018195397A2. |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
|