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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1320346-97-1
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2831.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1200.0 |
| 规格： | 5 mg | 产品价格： | ￥2160.0 |
| 规格： | 10 mg | 产品价格： | ￥3350.0 |
| 规格： | 25 mg | 产品价格： | ￥5360.0 |
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GLPG0187
CAS No. : 1320346-97-1
MCE 国际站：GLPG0187
产品活性：GLPG0187 是广谱的 integrin 受体拮抗剂，具有抗肿瘤活性；抑制 αvβ1-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。
研究领域：Cytoskeleton
作用靶点：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 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.
In Vivo: Blocking αv-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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