GLPG0187
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM[1]. GLPG0187 inhibits migrasome biogenesis without cytotoxicity[3].
Product Specifications
CAS Number
1320346-97-1
UNSPSC
12352005
Target
Integrin
Type
Reference compound
Related Pathways
Cytoskeleton
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GLPG0187.html
Purity
99.43
Solubility
DMSO : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)
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
Molecular Formula
C29H37N7O5S
Molecular Weight
595.71
References & Citations
[1]van der Horst G, et al. Targeting of α (v) -integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer. Neoplasia. 2011 Jun;13 (6) :516-25.|[2]Reeves KJ, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187. Int J Cancer. 2015 Apr 1;136 (7) :1731-40.|[3]Puzhong Lu, et al. Chemical screening identifies ROCK1 as a regulator of migrasome formation. Cell Discov. 2020 Aug 4;6 (1) :51.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Available Sizes
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