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Merck
CN

SML2526

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
NACRES:
NA.77
UNSPSC Code:
12352200

Key Documents

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Product Name

DDR-TRK-1, ≥98% (HPLC)

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

Quality Level

100

Biochem/physiol Actions

A chemical probe for the DDR and TRK kinase
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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000121836
0000121837
0000113165

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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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