GLPG0187

SKU: orb1303014

Description

GLPG0187 is a potent broad-spectrum integrin antagonist with an IC50 of 1.3 nM against αvβ1-integrin. This small molecule inhibitor is a valuable research tool for studying integrin function in fibrosis, cancer, and angiogenesis, applicable in both in vitro and in vivo experimental models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1320346-97-1
• MW: 595.71
• Purity: >99.99% (May vary between batches)
• Formula: C₂₉H₃₇N₇O₅S
• SMILES: COc1ccc(cc1)S(=O)(=O)N[C@@H](CNc1nc(C)nc(N2CCC(CC2)C2=CC=C3CCCN=C3N2)c1C)C(O)=O
• Target: Integrin
• Solubility: DMSO:13.38 mg/mL (22.46 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.68 mM)

Bioactivity

• Target IC50:
  αvβ1 integrin:1.3 nM
• In Vivo:
  GLPG0187 obviously reduces their metastatic tumor growth by blocking αv-integrins. GLPG0187 markedly lows Bone tumor burden and markedly inhibits the number of bone metastases/mouse. The progression of bone metastases and the formation of new bone metastases during the treatment period is significantly inhibited by GLPG0187.
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• In Vitro:
  GLPG0187 is an effective inhibitor of osteoclastic bone resorption and angiogenesis. In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors (IC50s: 1.3/3.7/2.0/1.4/1.2/7.7 nM, for αvβ1/3/5/6/8 and α5β1). GLPG0187 dose-dependently increases the E-cadherin/vimentin ratio. GLPG0187 dose-dependently reduces the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells. GLPG0187 causes cell rounding and clumping. GLPG0187 dose-dependently and markedly reduces in tumor cell migration. At all concentrations, GLPG0187 markedly reduces cell proliferation.
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• Cell Research:
  Tumour cell proliferation is determined using the MTS assay. PC3 cells are seeded at 10,000 cells/well in 96 well plates containing either GLPG0187 (0.5, 5, or 50 ng/mL), vehicle or media control, then cultured in 100 μL medium for 24 hr. Cell proliferation is analyzed using 20 μL MTS dye incubated for 3 hr at 37°C in the dark. Absorbance from each well (6/treatment) is quantified at 490 nm and the mean fluorescence calculated. The assay is repeated at 48, 72 and 96 hr, on three independent occasions.
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• Animal Research:
  GLPG0187 is prepared in 1:1 dimethyl sulfoxide in PBS.The effect of GLPG0187 on bone loss is evaluated in 3-month-old castrated male mice after 4 weeks of treatment with dosing starting immediately after castration (preventive protocol). Two different modes of administration are used: either subcutaneous twice daily with 10, 30, or 100 mg/kg of GLPG0187, either oral, twice daily with 30, 100, or 300 mg/kg of GLPG0187.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GLPG 0187, GLPG0187, GLPG-0187, Inhibitor, Integrin, inhibit, αvβ1 integrin

Compound Identifiers

PubChem CID

53340771