DDR1-IN-1 (hydrate)

The discoidin domain receptor (DDR) tyrosine kinases are activated by matrix collagens and are important for cell proliferation, differentiation, adhesion, migration, and invasion. DDR1-IN-1 binds to DDR1 and inhibits DDR1 autophosphorylation with an IC50 value of 105 nM and an EC50 value of 87 nM. It demonstrates weaker inhibition for DDR2 (IC50 = 413 nM) and has a good selectivity profile against a panel of 451 kinases. DDR-IN-1 has been shown to inhibit colorectal cancer cell lines when used in combination with the PI3K/mTOR inhibitor, GSK2126458 .