| Identification | Back Directory | [Name]
Pyrazolo[1,5-a]pyrimidin-7-amine, 5-(5-fluoro-3-pyridinyl)-N-[2-(1H-indol-3-yl)ethyl]-3-methyl- | [CAS]
2247950-73-6 | [Synonyms]
Pyrazolo[1,5-a]pyrimidin-7-amine, 5-(5-fluoro-3-pyridinyl)-N-[2-(1H-indol-3-yl)ethyl]-3-methyl- | [Molecular Formula]
C22H19FN6 | [MOL File]
2247950-73-6.mol | [Molecular Weight]
386.42 |
| Hazard Information | Back Directory | [Uses]
KYN-101 is a potent, selective and orally active AHR inhibitor. KYN-101 decreases the CYP1A1 mRNA expression. KYN-101 shows anti-cancer activity[1]. | [in vivo]
KYN-101 (10 mg/kg; p.o.; daily for 12 days) shows anti-cancer activity in mice[1]. | Animal Model: | 6-8 weeks, C57BL/6J mice (B16IDO tumor-bearing mice)[1] | | Dosage: | 10 mg/kg | | Administration: | P.o.; daily for 12 days | | Result: | Reduced tumor growth in B16IDO tumor-bearing mice and combination of KYN-101 and anti-PD-1 led to improved tumor growth delay and extended survival in CT26 models. |
| [References]
[1] Campesato LF, et al. Blockade of the AHR restricts a Treg-macrophage suppressive axis induced by L-Kynurenine. Nat Commun. 2020 Aug 11;11(1):4011. DOI:10.1038/s41467-020-17750-z |
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