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GLPG0187

CAS No. : 1320346-97-1

產品活性：GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits α_vβ₁-integrin with an IC₅₀ of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.

研究領域：Cytoskeleton

作用靶點：Integrin

In Vitro: In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors with IC₅₀s of 1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM for α_vβ₁, α_vβ₃, α_vβ₅, α_vβ₆,α_vβ₈, and α₅β₁. GLPG0187 is a potent inhibitor of osteoclastic bone resorption and angiogenesis. Treatment with GLPG0187 dose-dependently increases the E-cadherin/vimentin ratio, rendering the cells a more epithelial, sessile phenotype. GLPG0187 dose-dependently diminishes the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells. GLPG0187 treatment results in cell rounding and clumping. GLPG0187 demonstrates a dose-dependent significant reduction in tumour cell migration. GLPG0187 at all concentrations significantly reduces cell proliferation.

In Vivo: Blocking α_v-integrins by GLPG0187 markedly reduces their metastatic tumor growth. Bone tumor burden is significantly lower and the number of bone metastases/mouse is significantly inhibited. The progression of bone metastases and the formation of new bone metastases during the treatment period is significantly inhibited.

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