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| | Pyrazolo[1,5-a]pyrimidin-7-amine, 5-(5-fluoro-3-pyridinyl)-N-[2-(1H-indol-3-yl)ethyl]-3-methyl- Basic information |
| | Pyrazolo[1,5-a]pyrimidin-7-amine, 5-(5-fluoro-3-pyridinyl)-N-[2-(1H-indol-3-yl)ethyl]-3-methyl- Chemical Properties |
| density | 1.37±0.1 g/cm3(Predicted) | | pka | 17.14±0.30(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | Pyrazolo[1,5-a]pyrimidin-7-amine, 5-(5-fluoro-3-pyridinyl)-N-[2-(1H-indol-3-yl)ethyl]-3-methyl- Usage And Synthesis |
| 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 |
| | Pyrazolo[1,5-a]pyrimidin-7-amine, 5-(5-fluoro-3-pyridinyl)-N-[2-(1H-indol-3-yl)ethyl]-3-methyl- Preparation Products And Raw materials |
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