GLPG 0187
Chemical Name: 3-[[2,5-Dimethyl-6-[4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)-1-piperidinyl]-4-pyrimidinyl]amino]-N-[(4-methoxyphenyl)sulfonyl]-L-alanine
Purity: ≥97%
Biological Activity
GLPG 0187 is a potent αv integrin inhibitor (IC50 values are 1.2-3.7 nM). Inhibits osteoclastic bone resorption and angiogenesis in vitro and in vivo. Suppresses epithelial-mesenchymal transition (EMT) and migration of PC-3M-Pro4/luc cells, without inhibiting cell growth. Induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Targeting of αv-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer.
van der Horst, et al.
Neoplasia, 2011;13:516 -
Integrin inhibition promotes atypical anoikis in glioma cells.
Silginer et al.
Cell Death Dis., 2014;5:e1012
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