ROR1 inhibitor 24d is a potent, selective inhibitor of receptor tyrosine kinase-like orphan receptor ROR with IC50 of 17.6 nM.
ROR1 inhibitor 24d shows no activity against ROR2 (a homologous subtype of ROR1), also exhibits favorable selectivity on kinase profiling (126-kinase panel).
ROR1 inhibitor 24d demonstrates potent growth inhibition in ROR1-overexpressing cancer cell lines, including lung cancer cells (A549 and H1975) and breast cancer cells (MDA-MB-231) with IC50 of 0.47-0.64 uM.
ROR1 inhibitor 24d outperforms LDR102 in both kinase inhibition and cellular efficacy.
ROR1 inhibitor 24d effectively reduced colony formation in H1975, A549, and MDA-MB-231 cells in a dose-dependent manner.
ROR1 inhibitor 24d inhibited ROR1 downstream AKT/mTOR and NF-κB signaling pathways, ROR1 inhibitor 24d (5 uM) significantly reduced phospho-p65 levels in A549, MDA-MB-231, and H1975 cells.
ROR1 inhibitor 24d (5 mg/kg) demonstrates in vivo antitumor activity in A549 mouse xenograft models.