Product Details
| Product Name:
GLPG0187 |
CAS No.:
1320346-97-1 |
| Purity:
99.12% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | GLPG0187 |
| Description | GLPG0187, a broad spectrum integrin receptor antagonist, inhibits αvβ1-integrin (IC50: 1.3 nM). |
| 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. |
| 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 |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 5.96 mg/mL (10 mM)
|
| Keywords | inhibit | GLPG-0187 | GLPG0187 | Inhibitor | Integrin | GLPG 0187 |
| Inhibitors Related | K34c hydrochloride | E7820 | Arg-Gly-Asp TFA (99896-85-2(free base)) | Tirofiban hydrochloride monohydrate | Lifitegrast | Elarofiban TFA | Cyclo(-RGDfK) | Tirofiban | Bestatin hydrochloride | RO0270608 | ICAM-1-IN-1 | Gantofiban |
| Related Compound Libraries | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States