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Chemical Structure| 1320346-97-1 Chemical Structure| 1320346-97-1

Structure of GLPG0187
CAS No.: 1320346-97-1

Chemical Structure| 1320346-97-1

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GLPG 0187 is a potent αv integrin inhibitor with IC50 values of 1.2-3.7 nM. It inhibits osteoclastic bone resorption and angiogenesis in vitro and in vivo. Also it suppresses epithelial-mesenchymal transition (EMT) and migration of PC-3M-Pro4/luc cells, without inhibiting cell growth.

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Product Details of GLPG0187

CAS No. :1320346-97-1
Formula : C29H37N7O5S
M.W : 595.71
SMILES Code : O=C(O)[C@H](CNC1=NC(C)=NC(N2CCC(C3=NC4=C(CCCN4)C=C3)CC2)=C1C)NS(=O)(C5=CC=C(OC)C=C5)=O
MDL No. :MFCD31381920

Safety of GLPG0187

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of GLPG0187

cytoskeleton

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SMA-560 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.
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. Arterioscler Thromb Vasc Biol. 2023 Jul;43(7):1134-1153.
iPSC-derived SHF SMCs 10nM 24 h GLPG0187 significantly decreased p-FAK and p-AktThr308 signaling and inhibited cell proliferation and migration. Arterioscler Thromb Vasc Biol. 2023 Jul;43(7):1134-1153.
MDA-MB-231 cells 1 ng/ml 6 h pretreatment 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.

In Vivo:

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. Arterioscler Thromb Vasc Biol. 2023 Jul;43(7):1134-1153.
Zebrafish Zebrafish embryo xenograft model Added to zebrafish egg water 0.5 ng/ml Refreshed every second day, for 5 days 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. Breast Cancer Res. 2015 Feb 25;17(1):28.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01313598 Solid Tumors PHASE1 COMPLETED 2025-06-13 Nationaal Kanker Instituut (NK... More >>I), Amsterdam, 1066 CX, Netherlands|Universitair Medisch Centrum, Utrecht, 3584 CX, Netherlands Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.68mL

0.34mL

0.17mL

8.39mL

1.68mL

0.84mL

16.79mL

3.36mL

1.68mL

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