Name | DDR1-IN-1 dihydrochloride |
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Description | DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM)[1]. |
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Related Catalog | |
Target |
DDR1:105 nM (IC50) DDR2:413 nM (IC50) |
In Vitro | DDR1-IN-1 effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture[1]. |
References |
Molecular Formula | C30H33Cl2F3N4O3 |
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Molecular Weight | 625.51 |