DDR1-IN-1 dihydrochloride

Names

[ Name ]:
DDR1-IN-1 dihydrochloride

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Discoidin Domain Receptor

[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]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₀H₃₃Cl₂F₃N₄O₃

[ Molecular Weight ]:
625.51

DDR1-IN-1 dihydrochloride

Names

Biological Activity

Chemical & Physical Properties

Related Compounds