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Merck
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Key Documents

SML2526

Sigma-Aldrich

DDR-TRK-1

≥98% (HPLC)

别名:

(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

经验公式(希尔记法):
C26H23F3N6O
分子量:
492.50
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

光學活性

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

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

生化/生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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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