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DDR1-IN-1

Names

[ CAS No. ]:
1449685-96-4

[ Name ]:
DDR1-IN-1

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

DDR1 Inhibitor 7rh | DDR Inhibitor | DDR1-IN-3

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
609.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C30H31F3N4O3

[ Molecular Weight ]:
552.587

[ Flash Point ]:
322.1±31.5 °C

[ Exact Mass ]:
552.234802

[ LogP ]:
4.70

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.602

[ Storage condition ]:
-20℃


Related Compounds