ChemicalBook CAS DataBase List 1934246-19-1

1934246-19-1

Name	DDR-TRK-1 (DDR1 inhibitor 6j)
CAS	1934246-19-1
Molecular Formula	C26H23F3N6O
MDL Number	MFCD30543426
Molecular Weight	492.5
MOL File	1934246-19-1.mol

Chemical Properties

Boiling point	609.3±55.0 °C(Predicted)
density	1.37±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	powder
pka	12.84±0.70(Predicted)
color	white to beige
Optical Rotation	[α]/D -25 to -20°, c =0.5 in methanol

Safety Data

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Hazard Information

Uses

DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.

Biological Activity

DDR-TRK-1 was shown to inhibit the kinase activity of Discoidin Domain Receptor 1 (DDR1) with an IC50 value of 9.4 nM. DDR receptors are linked to the progression of various human diseasesincluding fibrotic disorders such as pulmonary fibrosisas well as atherosclerosis and cancer. DDR-TRK-1 showed a therapeutic effect in a mouse model of pulmonary fibrosis and inhibited Panc-1 pancreatic cancer cell colony formation and migration. DDR-TRK-1 also inhibits the TRK family kinases TRKATRKBand TRKCwhich are selectively expressed in neuronal tissue. DDR-TRK-1N is the negative control compound.

in vivo

DDR-TRK-1 prevents these BLM-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrotic markers in lung tissue lysates, including fibronectin and α-smooth muscle actin (SMA). Further analyses also reveal that the administration of DDR-TRK-1 cause a dose-dependent suppression in the content of hydroxyproline, a unique amino acid found in collagen. The above data collectively indicate the promising therapeutic potential of DDR-TRK-1 against the BLM-induced pulmonary fibrosis^[1].

storage

Store at -20°C

References

[1] Zhen Wang, et al. Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J Med Chem. 2016 Jun 23; 59(12): 5911–5916. DOI:10.1021/acs.jmedchem.6b00140

Spectrum Detail

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