DDR1-IN-6 is a potent and selective inhibitor of Discoidin Domain Receptor family member 1 (DDR1), exhibiting remarkable inhibitory activity at an IC50 of 9.72 nM. It effectively suppresses the auto-phosphorylation of DDR1b (Y513) with an IC50 value of 9.7 nM. Furthermore, DDR1-IN-6 displays strong anti-cancer activity.

DDR1:9.72 nM (IC50)

DDR1-IN-6 (compound 1), when applied for 24 hours, effectively inhibits collagen production in the human hepatic stellate cell line LX-2, with an IC50 value of 13 nM. Additionally, after 72 hours of exposure, DDR1-IN-6 exhibits cytotoxic effects on LX-2 cells, with a CC50 value of 3 μM. Furthermore, DDR1-IN-6 demonstrates anti-proliferative activity against primary tumor cells freshly isolated from PC-07-0024, achieving IC50 values of 5.7 μM after 3 days and 2.65 μM after 6 days. However, in a LU-01-0523 derived xenograft (PDX) tumor model, DDR1-IN-6 shows limited efficacy, with IC50 values exceeding 30 μM for both 3 and 6 days of treatment.