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GLPG0187

Catalog No. T4259 CAS 1320346-97-1

GLPG0187, a broad spectrum integrin receptor antagonist, inhibits αvβ1-integrin (IC50: 1.3 nM).

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GLPG0187, CAS 1320346-97-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
5 mg	In stock	$ 105.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 389.00
100 mg	In stock	$ 579.00
500 mg	In stock	$ 1,260.00
1 mL * 10 mM (in DMSO)	In stock	$ 138.00

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Purity: 99.12%

Purity: 99.01%

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Description	GLPG0187, a broad spectrum integrin receptor antagonist, inhibits αvβ1-integrin (IC50: 1.3 nM).
Targets&IC50	αvβ1:1.3 nM
In vitro	GLPG0187 is an effective inhibitor of osteoclastic bone resorption and angiogenesis. In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors (IC50s: 1.3/3.7/2.0/1.4/1.2/7.7 nM, for αvβ1/3/5/6/8 and α5β1). GLPG0187 dose-dependently increases the E-cadherin/vimentin ratio. GLPG0187 dose-dependently reduces the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells. GLPG0187 causes cell rounding and clumping. GLPG0187 dose-dependently and markedly reduces in tumor cell migration. At all concentrations, GLPG0187 markedly reduces cell proliferation.
In vivo	GLPG0187 obviously reduces their metastatic tumor growth by blocking αv-integrins. GLPG0187 markedly lows Bone tumor burden and markedly inhibits the number of bone metastases/mouse. The progression of bone metastases and the formation of new bone metastases during the treatment period is significantly inhibited by GLPG0187.
Kinase Assay	HSP90 competition isothermal calorimetry: Kd values for AT13387 binding to HSP90 are determined with a competition Isothermal Calorimetry (ITC) format. ITC experiments are performed on a Micro Cal VP-ITC at 25 °C in a buffer comprising 25 mM Tris, 100 mM NaCl, 1 mM MgCl2 and 1 mM Tris(2-carboxy- ethyl)phosphine at pH 7.4 in order to maintain the higher affinit
Cell Research	Tumour cell proliferation is determined using the MTS assay. PC3 cells are seeded at 10,000 cells/well in 96 well plates containing either GLPG0187 (0.5, 5, or 50 ng/mL), vehicle or media control, then cultured in 100 μL medium for 24 hr. Cell proliferation is analyzed using 20 μL MTS dye incubated for 3 hr at 37°C in the dark. Absorbance from each well (6/treatment) is quantified at 490 nm and the mean fluorescence calculated. The assay is repeated at 48, 72 and 96 hr, on three independent occasions.
Animal Research	GLPG0187 is prepared in 1:1 dimethyl sulfoxide in PBS.The effect of GLPG0187 on bone loss is evaluated in 3-month-old castrated male mice after 4 weeks of treatment with dosing starting immediately after castration (preventive protocol). Two different modes of administration are used: either subcutaneous twice daily with 10, 30, or 100 mg/kg of GLPG0187, either oral, twice daily with 30, 100, or 300 mg/kg of GLPG0187.

Molecular Weight	595.71
Formula	C29H37N7O5S
CAS No.	1320346-97-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.96 mg/mL (10 mM)

References and Literature

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 GLPG20187. Int J Cancer. 2015 Apr 1;136(7):1731-40.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Bioactive Compound Library Cytoskeletal Signaling Pathway Compound Library Orally Active Compound Library Clinical Compound Library Bioactive Compounds Library Max

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Keywords

GLPG0187 1320346-97-1 Cytoskeletal Signaling Integrin inhibit GLPG-0187 Inhibitor GLPG 0187 inhibitor

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