GLPG0187 - Integrin Antagonist - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGLPG0187Cat. No.: HY-100506CAS No.: 1320346-97-1分式: CHNOS分量: 595.71作靶點: Integrin作通路: Cytoskeleton儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 15 mg/mL (25.18 mM; Need ultrasonic and warm

2、ing)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6787 mL 8.3933 mL 16.7867 mL5 mM 0.3357 mL 1.6787 mL 3.3573 mL10 mM 0.1679 mL 0.8393 mL 1.6787 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 GLPG0187譜的integrin受體拮抗劑，具有抗腫瘤活性；抑制v1-integrin的IC50值為1.3 nM。IC50 & Target IC50:

3、1.3 nM (v1) 1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 v1, v3, v5, v6,v8, and 51. GLPG0187 is a potent inhibitor ofosteoclastic bone resorption and angiogenesis. Treatment with GLPG0187 dose-dependently

4、increases the1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEE-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 cells1. GLPG0187 treatment results in c

5、ell rounding and clumping. GLPG0187 demonstrates a dose-dependentsignificant reduction in tumour cell migration. GLPG0187 at all concentrations significantly reduces cellproliferation 2.體內(nèi)研究 Blocking v-integrins by GLPG0187 markedly reduces their metastatic tumor growth. Bone tumor burden issignific

6、antly lower and the number of bone metastases/mouse is significantly inhibited. The progression ofbone metastases and the formation of new bone metastases during the treatment period is significantlyinhibited 1.PROTOCOLCell Assay 2 Tumour cell proliferation is determined using the MTS assay. PC3 cel

7、ls are seeded at 10,000 cells/well in 96well plates containing either GLPG0187 (0.5, 5, or 50 ng/mL), vehicle or media control, then cultured in 100L medium for 24 hr. Cell proliferation is analysed using 20 L MTS dye incubated for 3 hr at 37C in thedark. Absorbance from each well (6/treatment) is q

8、uantified at 490 nm and the mean fluorescence calculated.The assay is repeated at 48, 72 and 96 hr, on three independent occasions 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: The effect of GLPG0187 on bone loss is evaluated in 3-month

9、-old castrated male mice after 4 weeks ofAdministration 1 treatment with dosing starting immediately after castration (preventive protocol). Two different modes ofadministration are used: either subcutaneous twice daily with 10, 30, or 100 mg/kg of GLPG0187, either oral,twice daily with 30, 100, or

10、300 mg/kg of GLPG0187 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. van der Horst G, et al. Targeting of (v)-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis inhuman 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. IntJ Cancer. 2015 Apr 1;136(7):1731-40.McePdfHeightCaution: Product has not been