GLPG0187 |
Catalog No.GC19167
One-Click Copy Product Info
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GLPG0187 is a broad-spectrum integrin receptor antagonist that exhibits selectivity for various integrin receptors, with the following IC50 values: αVβ1 at 1.3nM, αVβ3 at 3.7nM, αVβ5 at 2.0nM, αVβ6 at 1.4nM, αVβ8 at 1.2nM, and α5β1 at 7.7nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1320346-97-1
Sample solution is provided at 25 µL, 10mM.
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GLPG0187 is a broad-spectrum integrin receptor antagonist that exhibits selectivity for various integrin receptors, with the following IC50 values: αVβ1 at 1.3nM, αVβ3 at 3.7nM, αVβ5 at 2.0nM, αVβ6 at 1.4nM, αVβ8 at 1.2nM, and α5β1 at 7.7nM[1, 2]. GLPG0187 possesses anti-tumor activity, blocking the αvβ6 integrin receptor on cancer cells, locally preventing TGF-β activation, thereby reducing TGF-β signaling and immune evasion in cancer cells[3].
In vitro, GLPG0187 (20nM, 100nM, 200nM, 1µM) pretreatment of human small airway epithelial cells (HSAE) for 2h blocked SARS-CoV-2 delta and Omicron pseudovirus infection of airway epithelial cells in a dose-dependent manner[4]. Treatment of TALL-104 T lymphoblast cells with GLPG0187 (4µM) for 24h significantly enhanced the killing effect of TALL-104 T lymphoblast cells on HCT116 p53-null cells[5].
In vivo, GLPG0187 (100mg/kg) administered via intraperitoneal injection for 17 days in a mouse model of prostate cancer bone metastasis significantly reduced the number of tumor cells in the implanted metatarsal bones of the mice, significantly increased the number of osteoblasts, and significantly decreased microvessel density[6].
References:
[1] van der Horst G, van den Hoogen C, Buijs J T, et al. Targeting of αv-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer[J]. Neoplasia, 2011, 13(6): 516-IN9.
[2] Zhao-He L I, You Z, You-Xiang D, et al. Roles of integrin in tumor development and the target inhibitors[J]. Chinese journal of natural medicines, 2019, 17(4): 241-251.
[3] MacDonald W J, Verschleiser B, Carlsen L, et al. Broad spectrum integrin inhibitor GLPG-0187 bypasses immune evasion in colorectal cancer by TGF-β signaling mediated downregulation of PD-L1[J]. American Journal of Cancer Research, 2023, 13(7): 2938.
[4] Huntington K E, Carlsen L, So E Y, et al. Integrin/TGF-β1 inhibitor GLPG-0187 blocks SARS-CoV-2 delta and omicron pseudovirus infection of airway epithelial cells in vitro, which could attenuate disease severity[J]. Pharmaceuticals, 2022, 15(5): 618.
[5] Verschleiser B, MacDonald W, Carlsen L, et al. Pan-integrin inhibitor GLPG-0187 promotes T-cell killing of mismatch repair-deficient colorectal cancer cells by suppression of SMAD/TGF-β signaling[J]. American Journal of Cancer Research, 2023, 13(7): 2878.
[6] Reeves K J, Hurrell J E, Cecchini M, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187[J]. International journal of cancer, 2015, 136(7): 1731-1740.
| Cell experiment [1]: | |
Cell lines | Human small airway epithelial (HSAE) |
Preparation Method | HSAE cells were pre-treated with 20nM, 100nM, 200nM, or 1µM GLPG0187 for 2h followed by spin infection with either a pseudovirus expressing the D614G spike protein variant or a VsVg positive control for 24h. |
Reaction Conditions | 20nM, 100nM, 200nM, 1µM; 2h |
Applications | Pre-treatment with GLPG0187 resulted in the most significant decrease in pseudovirus infection by the Delta variant. |
| Animal experiment [2]: | |
Animal models | Server combined immune-deficiency (SCID) mouse |
Preparation Method | A single murine metatarsal was engrafted into a dorsal skinfold chamber implanted on a SCID mouse. Fluorescently-labeled human prostate (PC3-GFP) cancer cells were administered via intracardiac (i.c) injection. Animals were administered GLPG0187 daily for 17 days (i.p 100mg/kg; n=20, dissolved in 2% DMSO in PBS) or vehicle control (2% DMSO in PBS n=20), commencing on the same day as tumour cell injection (day 7). Metatarsal recordings were taken every 48h for up to 4 weeks. At the end of treatment animals were culled (day 25). Tissue was harvested and processed for microCT, multiphoton analysis, histology and immunohistochemistry. |
Dosage form | 100mg/kg; 17 days; i.p. |
Applications | GLPG0187 significantly reduced the number of tumour cells present in the implanted metatarsal from day 17 onwards. The number of osteoblasts was significantly increased in mice treated with GLPG0187. The microvessel density in the GLPG0187 treatment group was significantly lower compared to the control group. |
References: | |
| Cas No. | 1320346-97-1 | SDF | |
| Canonical 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 | ||
| Formula | C29H37N7O5S | M.Wt | 595.71 |
| Solubility | DMSO : 15 mg/mL (25.18 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6787 mL | 8.3933 mL | 16.7867 mL |
| 5 mM | 335.7 μL | 1.6787 mL | 3.3573 mL |
| 10 mM | 167.9 μL | 839.3 μL | 1.6787 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)