GLPG0187 induced detachment and the formation of large cell aggregates in GL-261 and SMA-560 NS cells, but no morphological changes were observed in SC cultures.
Cell Death Dis. 2014 Jan 23;5(1):e1012.
GL-261 mouse glioma cells
1 nM
24 h
GLPG0187 induced detachment and the formation of large cell aggregates in GL-261 and SMA-560 NS cells, but no morphological changes were observed in SC cultures.
Cell Death Dis. 2014 Jan 23;5(1):e1012.
PC-3M-Pro4/luc prostate cancer cells
0.39–200 nM
5 days
To evaluate the effect of GLPG0187 on osteoclast differentiation. GLPG0187 significantly decreased the amount of osteoclasts forming a ring, a structure necessary for osteoclastic resorption.
Neoplasia. 2011 Jun;13(6):516-25.
iPSC-derived NC SMCs
10nM
24 h
GLPG0187 reduced p-FAK and p-AktThr308 signaling, but the effect was less pronounced compared to SHF SMCs.
To investigate the effect of GLPG0187 on breast cancer cell migration, results showed that GLPG0187 pretreatment significantly reduced tumor cell invasion in the zebrafish model.
Breast Cancer Res. 2015 Feb 25;17(1):28.
MDA-MB-231 cells
0.5 or 1 ng/ml
48 h
To evaluate the effect of GLPG0187 on cell proliferation/viability, results showed that GLPG0187 treatment did not significantly change the proliferation rate of MDA-MB-231 cells.
Breast Cancer Res. 2015 Feb 25;17(1):28.
Human bronchial epithelial cells (16HBECs)
2 µM, 5 µM, 10 µM
12 h, 24 h, 48 h
GLPG0187 significantly increased the expression of E-cadherin and decreased the expression of mesenchymal markers like fibronectin and α-SMA, inhibiting TGF-β1-mediated EMT, proliferation, and migration in 16HBECs.
Front Immunol. 2023 Nov 1;14:1167605.
TNBC cell lines
2.5 µM
72 h
To assess the sensitivity of GLPG0187 in TNBC cell lines, showing consistent sensitivity profiles with cilengitide.
Breast Cancer Res. 2024 Dec 20;26(1):187.
GLPG0187 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
Prostate cancer bone metastasis model
Oral
30 or 100 mg/kg
Once daily for 15 days
To evaluate the therapeutic effect of GLPG0187 on existing bone metastases. GLPG0187 significantly inhibited the progression of bone metastases and significantly inhibited the formation of new bone metastases during the treatment period.
Neoplasia. 2011 Jun;13(6):516-25.
Mice
Marfan syndrome mouse model
Intraperitoneal
100mg/kg
Once daily from age 6 to 14 weeks
GLPG0187 treatment reduced aortic root aneurysm growth, elastin fragmentation and normalized the FAK/AktThr308/mTORC1 pathway.
To evaluate the inhibitory effect of GLPG0187 on breast cancer invasion and micrometastasis in the zebrafish model, results showed that GLPG0187 significantly reduced tumor cell invasion and micrometastasis.
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