1449685-96-4

1449685-96-4 structure

Name: DDR1-IN-1
Chemical Name: N-[3-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzamide
CAS Number: 1449685-96-4
Molecular Formula: C₃₀H₃₁F₃N₄O₃
Molecular Weight: 552.587
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Discoidin Domain Receptor
Create Date: 2018-12-28 10:34:54
Modify Date: 2024-01-13 12:47:55
DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinaseinhibitor with IC50/EC50 of 105 nM/87 nM; 4-fold less potent for DDR2 (IC50= 413 nM).IC50 value: 105 nM [1]Target: DDR1We confirmed the observed binding to DDR1 using an enzymatic kinase assay employing the Lanthascreen technology. In this assay DDR1-IN-1 exhibits an IC50 of 105 nM against DDR1 and 413 nM against DDR2. DDR1-IN-1 and DDR1-IN-2 inhibited basal DDR1 autophosphorylation with an EC50 of 86 nM and 9 nM, respectively. Both DDR1-IN-1 and DDR1-IN-2 demonstrated weaker inhibition of DDR1 autophosphorylation in the absence of collagen stimulation.

Name	N-[3-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzamide
Synonyms	4-[(4-Ethyl-1-piperazinyl)methyl]-N-{4-methyl-3-[(2-oxo-2,3-dihydro-1H-indol-5-yl)oxy]phenyl}-3-(trifluoromethyl)benzamide Benzamide, N-[3-[(2,3-dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)- DDR1-IN-1

Description	DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinaseinhibitor with IC50/EC50 of 105 nM/87 nM; 4-fold less potent for DDR2 (IC50= 413 nM).IC50 value: 105 nM [1]Target: DDR1We confirmed the observed binding to DDR1 using an enzymatic kinase assay employing the Lanthascreen technology. In this assay DDR1-IN-1 exhibits an IC50 of 105 nM against DDR1 and 413 nM against DDR2. DDR1-IN-1 and DDR1-IN-2 inhibited basal DDR1 autophosphorylation with an EC50 of 86 nM and 9 nM, respectively. Both DDR1-IN-1 and DDR1-IN-2 demonstrated weaker inhibition of DDR1 autophosphorylation in the absence of collagen stimulation.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Discoidin Domain Receptor Research Areas >> Cancer
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.