ROR1-IN-3 (Compound 24d) is a potent and highly selective inhibitor of the ROR1 kinase, with an IC50 of 17.6 nM. It demonstrates significant antitumor activity and ROR1 inhibition both in vitro and in vivo, exhibiting strong antiproliferative effects. ROR1-IN-3 induces apoptosis in cancer cell lines and inhibits downstream AKT/mTOR and NF-κB signaling pathways. This compound is applicable for antitumor research.