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SML2526

Sigma-Aldrich

DDR-TRK-1

≥98% (HPLC)

Synonym(s):

(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoro-methyl)-phenylamino)-(5-methyl-3-(pyrimidin-5-yl)-3-aza-bicyclo[4.4.0]deca-1(6),7,9-trien-9-yl)-methanone, (4R)-1,2,3,4-Tetrahydro-4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-2-(5-pyrimidinyl)-7-isoquinolinecarboxamide

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About This Item

Empirical Formula (Hill Notation):
C26H23F3N6O
CAS Number:
1934246-19-1
Molecular Weight:
492.50
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -25 to -20°, c = 0.5 in methanol

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

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 diseases, including fibrotic disorders such as pulmonary fibrosis, as 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 TRKA, TRKB, and TRKC, which are selectively expressed in neuronal tissue. DDR-TRK-1N is the negative control compound.

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Zhen Wang et al.
Journal of medicinal chemistry, 59(12), 5911-5916 (2016-05-25)
The structure-based design of 1, 2, 3, 4-tetrahydroisoquinoline derivatives as selective DDR1 inhibitors is reported. One of the representative compounds, 6j, binds to DDR1 with a Kd value of 4.7 nM and suppresses its kinase activity with an IC50 value

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