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GLPG 0187

Cat. No. 7059 Submit a Review Datasheet / COA / SDS
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Description: Potent αv integrin inhibitor
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% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for GLPG 0187

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 for GLPG 0187

M. Wt 595.71
Formula C29H37N7O5S
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 1320346-97-1
PubChem ID 53340771
InChI Key CXHCNOMGODVIKB-VWLOTQADSA-N
Smiles 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

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.

Solubility Data for GLPG 0187

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.96 10

Preparing Stock Solutions for GLPG 0187

The following data is based on the product molecular weight 595.71. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 16.79 mL 83.93 mL 167.87 mL
0.5 mM 3.36 mL 16.79 mL 33.57 mL
1 mM 1.68 mL 8.39 mL 16.79 mL
5 mM 0.34 mL 1.68 mL 3.36 mL

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References for GLPG 0187

References are publications that support the biological activity of the product.

van der Horst, et al (2011) Targeting of αv-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer. Neoplasia 13 516 PMID: 21677875

Silginer et al (2014) Integrin inhibition promotes atypical anoikis in glioma cells. Cell Death Dis. 5 e1012 PMID: 24457956

If you know of a relevant reference for GLPG 0187, please let us know.

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Keywords: GLPG 0187, GLPG 0187 supplier, GLPG0187, αv, integrins, inhibitors, inhibitor, inhibits, inhibit, epithelial-mesenchymal, transition, EMT, osteoclastic, bone, resorption, Integrins, Cell, Adhesion, Molecules, 7059, Tocris Bioscience

Citations for GLPG 0187

Citations are publications that use Tocris products.

Currently there are no citations for GLPG 0187. Do you know of a great paper that uses GLPG 0187 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Enabling Research By Provision of Chemical Tools Poster

Enabling Research By Provision of Chemical Tools Poster

The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.