货号	规格	价格	上海	北京	珠海	重庆	武汉
S82829-1mg买3赠1	≥98%	￥510.00 S82829-1mg ￥510.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S82829-2mg买3赠1	99.90%	￥765.00 S82829-2mg ￥765.00 现货（买3赠1）	6 6	-	-	-	-
S82829-5mg买3赠1	99.90%	￥1060.00 S82829-5mg ￥1060.00 现货（买3赠1）	5 5	-	-	-	-
S82829-10mg买3赠1	99.90%	￥1610.00 S82829-10mg ￥1610.00 现货（买3赠1）	3 3	-	-	-	-
S82829-50mg	99.90%	￥5860.00 S82829-50mg ￥5860.00 现货	2 2	-	-	-	-
S82829-100mg	≥98%	￥10200.00 S82829-100mg ￥10200.00 2-3天	0 货期：2-3天	-	-	-	-

大包装询价收藏产品

加入购物车

产品描述：

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity

靶点：

IC50: 1.3 nM (αvβ1);Integrin

体外研究：

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.

体内研究：

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

参考文献：

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. 3. Puzhong Lu, et al. Chemical screening identifies ROCK1 as a regulator of migrasome formation. Cell Discov. 2020 Aug 4;6(1):51.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.679 ml	8.393 ml	16.787 ml
5 mM	0.336 ml	1.679 ml	3.357 ml
10 mM	0.168 ml	0.839 ml	1.679 ml
50 mM	0.034 ml	0.168 ml	0.336 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置