An αν integrin receptor antagonist
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GLPG0187

Item No. 21792

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    GLPG0187 is a nonpeptide antagonist of αν integrin receptors (IC50s = 1.2-3.7 nM).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. van der Horst, G., van den Hoogen, C., Buijis, J.T., et al. Targeting of αν-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer. Neoplasia 13(6), 516-525 (2011).

    2. Silginer, M., Weller, M., Ziegler, U., et al. Integrin inhibition promotes atypical anoikis in glioma cells. Cell Death Dis. 5, e1012 (2014).