Description
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
Product information
Molecular Weight: 499.54
Formula: C54H52F2N14O4
Chemical 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 hemimaleate
Smiles: CC(C)C1C=NN2C=1N=C(N=C2N[C@H]1CC2C3=CC=CC=C3NC=2CC1)C1=CC(F)=CN=C1.CC(C)C1C=NN2C=1N=C(N=C2N[C@H]1CC2C3=CC=CC=C3NC=2CC1)C1=CC(F)=CN=C1.OC(=O)/C=C\C(O)=O
InChiKey: HTQJDFMOXLTXNH-ZNPSPWATSA-N
InChi: InChI=1S/2C25H24FN7.C4H4O4/c2*1-14(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;5-3(6)1-2-4(7)8/h2*3-6,9,11-14,17,30H,7-8,10H2,1-2H3,(H,29,31,32);1-2H,(H,5,6)(H,7,8)/b;;2-1-/t2*17-;/m11./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 Vitro:
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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