GLPG0187 是广谱的 integrin 受体拮抗剂，具有抗肿瘤活性；抑制 α_vβ₁-integrin 的 IC₅₀ 值为 1.3 nM。GLPG0187 抑制细胞迁移体生物合成而无细胞毒性。

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits α v β 1 -integrin with an IC 50 of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.

Solid

IC50: 1.3 nM (αvβ1)

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 αvβ1, αvβ3, αvβ5, αvβ6,αvβ8, 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.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. van der Horst G, et al. Targeting of α(v)-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer. Neoplasia. 2011 Jun;13(6):516-25.
[2]. Reeves KJ, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187. Int J Cancer. 2015 Apr 1;136(7):1731-40.

In Vitro: DMSO : 12.5 mg/mL (20.98 mM; ultrasonic and warming and heat to 60°C)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液