GLPG0187

GLPG0187 is a nonpeptide antagonist of alphanu integrin receptors (IC50s = 1.2-3.7 nM). It inhibits osteoclastogenesis, bone resorption, and angiogenesis in vitro and in vivo in mice, which are all hallmarks of bone marrow invasion in metastatic prostate cancer. GLPG0187 reduces epithelial-mesenchymal transition (EMT) and migration of PC-3M-Pro4/luc cells in a dose-dependent manner without inhibiting cell growth. GLPG0187 also induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells.Formal 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. CAS Number: 1320346-97-1. Molecular Formula: C29H37N7O5S. Formula Weight: 595.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 3 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 240 nm. 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. InChi Code: 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. InChi Key: CXHCNOMGODVIKB-VWLOTQADSA-N.