1. Cytoskeleton
  2. Integrin

GLPG0187 

Cat. No.: HY-100506 Purity: 98.08%
Handling Instructions

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.

For research use only. We do not sell to patients.

GLPG0187 Chemical Structure

GLPG0187 Chemical Structure

CAS No. : 1320346-97-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 519 In-stock
Estimated Time of Arrival: December 31
1 mg USD 144 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 540 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.

IC50 & Target

IC50: 1.3 nM (αvβ1)[1]

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, αvβ6vβ8, 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[1]. 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[2].

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[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 15 mg/mL (25.18 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6787 mL 8.3933 mL 16.7867 mL
5 mM 0.3357 mL 1.6787 mL 3.3573 mL
10 mM 0.1679 mL 0.8393 mL 1.6787 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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 analysed 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

595.71

Formula

C₂₉H₃₇N₇O₅S

CAS No.

1320346-97-1

SMILES

O=C(O)[[email protected]](CNC1=NC(C)=NC(N2CCC(C3=NC4=C(CCCN4)C=C3)CC2)=C1C)NS(=O)(C5=CC=C(OC)C=C5)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GLPG0187
Cat. No.:
HY-100506
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GLPG0187

Cat. No.: HY-100506