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; for 24 hours) inhibits collagen production in human hepatic stellate cell LX-2 (IC 50 =13 nM)[1]. DDR1-IN-6 (72 hours) has cytotoxicity in LX-2 cells (CC 50 =3 μM)[1]. DDR1-IN-6 (0-30 μM) has anti-proliferation effects on primary tumor cells freshly isolated from PC-07-0024 (IC 50 =5.7 μM of 3 days; IC 50 =2.65 μM of 6 days) and LU-01-0523 derived xenograft (PDX) tumor model (IC 50 >30 μM of 3 days; IC 50 >30 μM of 6 days)[1].