| Name | GLPG0187 |
| Description | GLPG0187, a broad spectrum integrin receptor antagonist, inhibits αvβ1-integrin (IC50: 1.3 nM). |
| 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. |
| Kinase Assay | HSP90 competition isothermal calorimetry: Kd values for AT13387 binding to HSP90 are determined with a competition Isothermal Calorimetry (ITC) format. ITC experiments are performed on a Micro Cal VP-ITC at 25 °C in a buffer comprising 25 mM Tris, 100 mM NaCl, 1 mM MgCl2 and 1 mM Tris(2-carboxy- ethyl)phosphine at pH 7.4 in order to maintain the higher affinit |
| 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. |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.68 mM), Sonication is recommended.
DMSO : 13.38 mg/mL (22.46 mM), Sonication is recommended.
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| Keywords | αvβ1 integrin | Integrin | Inhibitor | inhibit | GLPG-0187 | GLPG0187 | GLPG 0187 |
| Inhibitors Related | K34c hydrochloride | Cucurbitacin B | Tirofiban hydrochloride monohydrate | (R)-Leucic acid | Lifitegrast | Cyclo(-RGDfK) | ADH-503 | Elsibucol | CLT-28643 | Bestatin hydrochloride | Gantofiban | 2-hydroxy Flutamide |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
