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Description: DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, and is about 3-fold selectivity over DDR2. DDR1-IN-1 binds to DDR1 in the 'DFG-out' conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity as assessed against a panel of 451 kinases measured. DDR1-IN-1 provides a useful pharmacological probe for DDR1-dependent signal transduction. The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion.
References: ACS Chem Biol. 2013 Oct 18; 8(10):2145-50.
Chemical Name: 4-((4-ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-(2-oxoindolin-5-yloxy)phenyl)-3-(trifluoromethyl)benzamide
SMILES: FC(C1=CC(C(NC2=CC=C(C(OC3=CC(C4)=C(C=C3)NC4=O)=C2)C)=O)=CC=C1CN5CCN(CC)CC5)(F)F
DDR1-IN-1; DDR1-IN 1; DDR1-IN1
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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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