ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 effectively inhibits aberrant ROR1 expression, which is associated with the development of non-small cell lung cancer (NSCLC) and EGFR-TKI-induced drug resistance. ARI-1 binds to the extracellular Frizzled domain of ROR1 and regulates PI3K/AKT/mTOR signaling in a ROR1-dependent manner. ARI-1 potently inhibits NSCLC cell proliferation and migration and has antitumor activity in vivo[1].
References:
[1]. Liu X, et al. Novel ROR1 inhibitor ARI-1 suppresses the development of non-small cell lung cancer. Cancer Lett. 2019 Aug 28,458:76-85.