DDR1-IN-1 |
| Katalog-Nr.GC17365 |
DDR1-IN-1 ist ein potenter und selektiver DDR1-Rezeptor-Tyrosinkinase-Inhibitor mit einem IC50 von 105 nM; 4-fach weniger potent fÜr DDR2 (IC50 = 413 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1449685-96-4
Sample solution is provided at 25 µL, 10mM.
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DDR1-IN-1 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].
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:
[1]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50.
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