ROR1-IN-1 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 ( ROR 1 ) with K i of 0.10 μM. ROR1-IN-1 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC 50 of 0.36 μM, 1.37 μM and 0.47 μM. ROR1-IN-1 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models.