1. Cytoskeleton
  2. Integrin
  3. GLPG0187

GLPG0187 

Cat. No.: HY-100506 Purity: 99.78%
COA Handling Instructions

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.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 519 In-stock
Solution
10 mM * 1 mL in DMSO USD 519 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 130 In-stock
10 mg USD 190 In-stock
50 mg USD 850 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GLPG0187 purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2023 Apr 20.  [Abstract]

    GLPG0187 (10 nM; 24 h) significantly reduces the expression of p-AktThr308 signaling in SHF and NC cells.

    GLPG0187 purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2023 Apr 20.  [Abstract]

    GLPG0187 (10 nM; 24 h) significantly reduces the expression of Ki-67 in SHF and NC cells.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM[1]. GLPG0187 inhibits migrasome biogenesis without cytotoxicity[3].

    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].

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

    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].

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

    Clinical Trial
    Molecular Weight

    595.71

    Formula

    C29H37N7O5S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (20.98 mM; ultrasonic and warming and heat to 60°C)

    H2O : < 0.1 mg/mL (insoluble)

    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  20% HP-β-CD in Saline

      Solubility: 10 mg/mL (16.79 mM); Suspension solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.25 mg/mL (2.10 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (2.10 mM); Clear solution

    • 4.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 0.89 mg/mL (1.49 mM); Clear solution

    • 5.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.89 mg/mL (1.49 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.78%

    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
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    GLPG0187 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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