Description
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.
Product information
CAS Number: 2247953-39-3
Molecular Weight: 550.89
Formula: C25H27Cl3FN7
Chemical Name: (3R)-N-[2-(5-fluoropyridin-3-yl)-8-(propan-2-yl)pyrazolo[1,5-a][1,3,5]triazin-4-yl]-2,3,4,9-tetrahydro-1H-carbazol-3-amine trihydrochloride
Smiles: Cl.Cl.Cl.CC(C)C1C=NN2C=1N=C(N=C2N[C@@H]1CCC2NC3=CC=CC=C3C=2C1)C1=CN=CC(F)=C1
InChiKey: SRGGKFXUJGRKIJ-NMRXSTGRSA-N
InChi: InChI=1S/C25H24FN7.3ClH/c1-14(2)20-13-28-33-24(20)31-23(15-9-16(26)12-27-11-15)32-25(33)29-17-7-8-22-19(10-17)18-5-3-4-6-21(18)30-22;;;/h3-6,9,11-14,17,30H,7-8,10H2,1-2H3,(H,29,31,32);3*1H/t17-;;;/m1.../s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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