DDR1-IN-1

Modify Date: 2024-01-13 12:47:55

DDR1-IN-1 Structure
DDR1-IN-1 structure
Common Name DDR1-IN-1
CAS Number 1449685-96-4 Molecular Weight 552.587
Density 1.3±0.1 g/cm3 Boiling Point 609.0±55.0 °C at 760 mmHg
Molecular Formula C30H31F3N4O3 Melting Point N/A
MSDS N/A Flash Point 322.1±31.5 °C

 Use of DDR1-IN-1


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.

 Names

Name N-[3-[(2,3-Dihydro-2-oxo-1H-indol-5-yl)oxy]-4-methylphenyl]-4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)benzamide
Synonym More Synonyms

 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
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

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℃

 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
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