Catalog No.: PC-24447Not For Human Use, Lab Use Only.
DDR1-IN-1 is a potent and selective inhibitor of DDR1 receptor tyrosine kinase with IC50 of 105 nM, 4-fold selective over DDR-2 (IC50=413 nM), inhibits DDR1 autophosphorylation in cells.
DDR1-IN-1 is a potent and selective inhibitor of DDR1 receptor tyrosine kinase with IC50 of 105 nM, 4-fold selective over DDR-2 (IC50=413 nM), inhibits DDR1 autophosphorylation in cells. DDR1-IN-1 exhibits excellent selectivity for DDR1 with a selectivity score (S(1) at 1 μM) of 0.01 as assessed using the KinomeScan approach. DDR1-IN-1 blocks collagen induced DDR1 autophosphorylation in U2OS cells with EC50 of 86 nM. DDR1-IN-1 binds to DDR1 in the 'DFG-out' conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity. Inhibitors of PI3K and mTOR such as GSK2126458 potentiate the antiproliferative activity of DDR1-IN-1 in colorectal cancer cell lines.
