GLPG0259
Based on 1 Customer Validation
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.63%
- No. CAS: 959754-85-9
- Fòrmula: C24H28N8O2
- Peso molecular:460.53
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
MAPK-activated protein kinase 5 (MK5)[1]
In Vitro
GLPG0259 reduces inflammation and release of bone degrading mediators, but did not affect phosphorylation of c-jun NH(2) -terminal protein kinase (JNK), ERK, and p38 MAP kinase[1].
GLPG0259 (1-5 μM; 48 h) leads to the reduction and remodeling of actin filamentation in prostate cancer (PCa) cell lines, LNCaP and PC3[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 959754-85-9
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Appearance Solid
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Peso molecular 460.53
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Fòrmula C24H28N8O2
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Color Off-white to yellow
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SMILES
O=C(C1=CC(C2=CN=C(NC3=CC=C(N4CCN(C(C)(C)C)CC4)C=C3)C5=NC=NN52)=CO1)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 3.33 mg/mL (7.23 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Westhovens R, et al. Oral administration of GLPG0259, an inhibitor of MAPKAPK5, a new target for the treatment of rheumatoid arthritis: a phase II, randomised, double-blind, placebo-controlled, multicentre trial. Ann Rheum Dis. 2013 May;72(5):741-4. [Content Brief]
[2]. Khalil MI, et al. The TLK1-MK5 Axis Regulates Motility, Invasion, and Metastasis of Prostate Cancer Cells. Cancers (Basel). 2022 Nov 22;14(23):5728. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL | 54.2853 mL |
| 5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL | 10.8571 mL |
GLPG0259 Related Classifications
HY-136990 Related Classifications
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