| 产品描述: | DDR抑制剂;DDR Inhibitors;;InformationDDR1-IN-1 DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2.TargetsDDR1 (Cell-free assay); DDR2 (Cell-free assay) 105 nM; 413 nMIn vitroIn U2OS cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with EC50 of 86 nM, and demonstrates stronger inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines that possess DDR1 gain-of-function mutations and/or overexpression, DDR1-IN-1, dose not inhibit proliferation below a concentration of 10 μM, while GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1.Cell Research(from reference)Cell lines:U2OSWT, U2OSOWT and U2OSG707A cell lines Concentrations:~20 μM Incubation Time:48 h |