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Merck
모든 사진(1)

Key Documents

SML2526

Sigma-Aldrich

DDR-TRK-1

≥98% (HPLC)

동의어(들):

(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

실험식(Hill 표기법):
C26H23F3N6O
CAS Number:
Molecular Weight:
492.50
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

광학 활성

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

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

생화학적/생리학적 작용

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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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