| Identification | Back Directory | [Name]
DDR-TRK-1
(DDR1 inhibitor 6j) | [CAS]
1934246-19-1 | [Synonyms]
DDR-TRK-1
DDR-TRK-1
(DDR1 inhibitor 6j)
7-Isoquinolinecarboxamide, 1,2,3,4-tetrahydro-4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-2-(5-pyrimidinyl)-, (4R)- | [Molecular Formula]
C26H23F3N6O | [MDL Number]
MFCD30543426 | [MOL File]
1934246-19-1.mol | [Molecular Weight]
492.5 |
| Chemical Properties | Back Directory | [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 activity]
[α]/D -25 to -20°, c =0.5 in methanol |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|