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GLPG0187 98%

GLPG0187

源葉(MedMol)
S82829
1320346-97-1
C29H37N7O5S
595.713
品牌 貨號 產品規格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數量
源葉(MedMol) S82829-1mg 98% ￥510.00元 預計交期：2-3天 - - -
源葉(MedMol) S82829-2mg 98% ￥765.00元 6 - - -
源葉(MedMol) S82829-5mg 98% ￥1062.50元 6 - - -
源葉(MedMol) S82829-10mg 98% ￥1615.00元 4 - - -
源葉(MedMol) S82829-50mg 98% ￥5865.00元 2 - - -
源葉(MedMol) S82829-100mg 98% ￥10200.00元 預計交期：2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

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
產品描述： 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
靶點： IC50: 1.3 nM (αvβ1);Integrin
體外研究：
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.
體內研究：
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
參考文獻：
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
保存條件： -20℃
配置溶液濃度參考：
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
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參考文獻

質檢證書(COA)

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批號：C10000001 貨號：A800001-25g
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摩爾濃度計算器

質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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