1,2-Benzisoxazol-3-amine, 7-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-6-methyl-N-[3-(trifluoromethyl)phenyl]-

Description

DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC₅₀ of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC₅₀ of 9.7 nM. DDR1-IN-6 has anti-cancer activity^[1].

DDR1-IN-6 (compound 1; for 24 hours) inhibits collagen production in human hepatic stellate cell LX-2 (IC₅₀=13 nM)^[1].
DDR1-IN-6 (72 hours) has cytotoxicity in LX-2 cells (CC₅₀=3 μM)^[1].
DDR1-IN-6 (0-30 μM) has anti-proliferation effects on primary tumor cells freshly isolated from PC-07-0024 (IC₅₀=5.7 μM of 3 days; IC₅₀=2.65 μM of 6 days) and LU-01-0523 derived xenograft (PDX) tumor model (IC₅₀>30 μM of 3 days; IC₅₀>30 μM of 6 days)^[1].