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].
KYN-101 (0.5, 1 µM; 24 h) 降低 IDOhigh 样本中的 CYP1A1 mRNA 表达[1]。
KYN-101 (10 mg/kg；口服；每日一次，持续 12 天) 在小鼠体内显示出抗癌活性[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. |
[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.