GLPG0187

• CAT Number: I006969
• CAS Number: 1320346-97-1
• Molecular Formula: C29H37N7O5S
• Molecular Weight: 595.7
• Purity: ≥95%
• Synonyms: GLPG0187; GLPG 0187; GLPG-0187;(S)-3-((2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin-1-yl)pyrimidin-4-yl)amino)-2-((4-methoxyphenyl)sulfonamido)propanoic acid.
• Target: integrin receptor antagonist
• Solubility: Soluble in DMSO, not in water
• Storage: -20°C
• InChI: InChI=1S/C29H37N7O5S/c1-18-26(31-17-25(29(37)38)35-42(39,40)23-9-7-22(41-3)8-10-23)32-19(2)33-28(18)36-15-12-20(13-16-36)24-11-6-21-5-4-14-30-27(21)34-24/h6-11,20,25,35H,4-5,12-17H2,1-3H3,(H,30,34)(H,37,38)(H,31,32,33)/t25-/m0/s1
• InChIKey: CXHCNOMGODVIKB-VWLOTQADSA-N
• SMILES: [H]N1C(C2CCN(C3=C(C)C(N([H])C[C@H](N([H])S(C4=CC=C(OC)C=C4)(=O)=O)C(O)=O)=NC(C)=N3)CC2)=CC=C5CCCN=C51

GLPG0187 is a small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity. Upon administration, GLPG0187 binds to and blocks the activity of 5 RGD-integrin receptor subtypes, including alphavbeta1, alphavbeta3, alphavbeta5, alphavbeta6 and alpha5beta1. This may result in the inhibition of endothelial cell-cell interactions and endothelial cell-matrix interactions, and the prevention of angiogenesis and metastasis in tumor cells expressing these integrin receptors. Integrin receptors are transmembrane glycoproteins expressed on the surface of tumor vessel endothelial cells and some types of cancer cells, and play a crucial role in endothelial cell adhesion and migration.

Reference

1:A dose escalating phase I study of GLPG0187, a broad spectrum integrin receptor antagonist, in adult patients with progressive high-grade glioma and other advanced solid malignancies. Cirkel GA, Kerklaan BM, Vanhoutte F, Van der Aa A, Lorenzon G, Namour F, Pujuguet P, Darquenne S, de Vos FY, Snijders TJ, Voest EE, Schellens JH, Lolkema MP.Invest New Drugs. 2016 Apr;34(2):184-92. doi: 10.1007/s10637-015-0320-9. Epub 2016 Jan 20. PMID: 26792581 Free PMC Article2:Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187. Reeves KJ, Hurrell JE, Cecchini M, van der Pluijm G, Down JM, Eaton CL, Hamdy F, Clement-Lacroix P, Brown NJ.Int J Cancer. 2015 Apr 1;136(7):1731-40. doi: 10.1002/ijc.29165. Epub 2014 Sep 4. PMID: 25156971 Free Article