DDR1-IN-1 exhibits potent and selective inhibition of the DDR1 receptor tyrosine kinase, with an IC50 of 105 nM. It is approximately four times less potent for DDR2, with an IC50 of 413 nM[1].
体外研究
In U2OS cells, DDR1-IN-1 effectively hinders collagen-induced DDR1 pY513 autophosphorylation, with an EC50 of 86.76 nM, demonstrating excellent selectivity over a panel of >380 kinases. Additionally, DDR1-IN-1 suppresses DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) following collagen stimulation, with an IC50 of less than 2.5 μM. Moreover, it enhances the antiproliferation efficacy of the PI3K/mTOR inhibitor GSK2126458 in SNU-1040 colorectal cancer culture[1].
Assess cell viability, DDR1-IN-1 drastically reduced cell viability within a narrow concentration range
Cell Death Discov. 2025 Mar 1;11(1):83.
SNU-449 cells
>10 μM
Anti-proliferation effect
ACS Chem Biol. 2013 Oct 18;8(10):2145-50.
EJ cells
>10 μM
Anti-proliferation effect
ACS Chem Biol. 2013 Oct 18;8(10):2145-50.
SNU-1040 cells
>10 μM
Anti-proliferation effect
ACS Chem Biol. 2013 Oct 18;8(10):2145-50.
SW480 cells
>10 μM
Anti-proliferation effect
ACS Chem Biol. 2013 Oct 18;8(10):2145-50.
Liver sinusoidal endothelial cells (LSECs)
70 nM
3 h
DDR1-IN-1 did not significantly modify MMPs secretion in LSECs.
Sci Rep. 2020 Oct 27;10(1):18398.
Kupffer cells (KCs)
70 nM
3 h
DDR1-IN-1 reduced the expression of active MMP9 in KCs but did not significantly affect total MMPs secretion.
Sci Rep. 2020 Oct 27;10(1):18398.
Hepatic stellate cells (HSCs)
70 nM
3 h
DDR1-IN-1 decreased MMP2 and MMP9 secretion in HSCs and reduced the promotion of LSECs and C26 cell migration and proliferation by HSC-derived factors.
Sci Rep. 2020 Oct 27;10(1):18398.
U2OS cells
105 nM
2 h
Evaluate the inhibitory effect of DDR1-IN-1 on collagen-induced DDR1 autophosphorylation
J Mol Biol. 2014 Jun 26;426(13):2457-70.
LN-229
4.99 µM
24 h
Investigation of the effect of DDR1-IN-1 on the radiosensitivity of glioblastoma cells, showing that DDR1-IN-1 combined with cilengitide significantly enhanced radiosensitivity.
Am J Cancer Res. 2023 Oct 15;13(10):4597-4612.
U-251MG
4.99 µM
24 h
Investigation of the effect of DDR1-IN-1 on the radiosensitivity of glioblastoma cells, showing that DDR1-IN-1 combined with cilengitide significantly enhanced radiosensitivity.
Am J Cancer Res. 2023 Oct 15;13(10):4597-4612.
DDR1-IN-1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c mice
Colon carcinoma liver metastasis model
Tail vein injection
1.5 mg/kg
Three consecutive days, once daily
DDR1 silencing reduced the number and size of metastatic foci in the liver and decreased collagen and MMPs activity in the tumor microenvironment.
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