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Filgotinib (GLPG0634) is an orally-available, selective inhibitor of JAK1 (Janus kinase 1) for the treatment of rheumatoid arthritis and potentially other inflammatory diseases. Filgotinib (GLPG0634) dose-dependently inhibited Th1 and Th2 differentiation and to a lesser extent the differentiation of Th17 cells in vitro. GLPG0634 was well exposed in rodents upon oral dosing, and exposure levels correlated with repression of Mx2 expression in leukocytes. The JAK1 selective inhibitor GLPG0634 (Filgotinib) is a promising novel therapeutic with potential for oral treatment of rheumatoid arthritis and possibly other immune-inflammatory diseases. Filgotinib (GLPG0634) is currently in a Phase 2 study in Crohn's disease.
Front Cell Dev Biol. 2021 Apr 15;9:665869.
Enhancing Fatty Acid Catabolism of Macrophages Within Aberrant Breast Cancer Tumor Microenvironment Can Re-establish Antitumor Function
Filgotinib purchased from AbMole
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Source | Front Cell Dev Biol (2021). Figure 6. Filgotinib (Abmole Bioscience, Houston, USA) |
| Method | cell culture | |
| Cell Lines | The TNBC cell lines MDA-MB-231 and MDA-MB-468 | |
| Concentrations | 1 µM | |
| Incubation Time | - | |
| Results | Filgotinib (JAK1-STAT1 inhibitor, 1 µM) abrogated SIRT1 expression in the CTRL group, while IFN-γ (JAK1-STAT1 agonist, 10 µg/mL) promoted SIRT1 expression in the Co-CM1 group |
| Cell Experiment | |
|---|---|
| Cell lines | T cells |
| Preparation method | T cell differentiation studies. PBMCs were isolated from buffy coats of healthy donors (Blood Transfusion Center, Red Cross, Leuven, Belgium) using density gradient centrifugation on Lymphoprep. Naive CD4+ T cells were further isolated by depletion of non–T helper and memory CD4+ T cells using a naive CD4+ T cell isolation kit II (Miltenyi Biotec). Isolated naive CD4+ T cells were stimulated with plate-bound anti-CD3 (3 μg/ml) and anti-CD28 (5 μg/ml) Abs in the presence of cytokines that drive differentiation into Th1, Th2, or Th17 Th subsets. For Th1 cell polarization, cells were cultured in the presence of 10 μg/ml anti–IL-4 Ab (MAB204; R&D Systems), 10 ng/ml IL-2 (R&D Systems), and 10 ng/ml IL-12 (R&D Systems) (17). For Th2 cell polarization, cells were cultured in the presence of 10 μg/ml anti–IFN-γ Ab (Becton Dickinson), 25 ng/ml IL-4 (R&D Systems), and 10 ng/ml IL-2 (17). For Th17 cell polarization, a mix of the following cytokines was used: 10 ng/ml IL-6 (R&D Systems), 10 ng/ml IL-1β (R&D Systems), 1 ng/ml TGF-β (PeproTech), and 100 ng/ml IL-23 (R&D Systems) (18). To monitor effects of compounds on T cell differentiation, compounds were added at indicated concentrations at the start of T cell differentiation. After 5 d, RNA was extracted using an RNeasy Mini kit (Qiagen), reverse transcribed, and the extent of Th subset differentiation was monitored by determining expression of IFN-γ (Th1 marker), IL-13 (Th2 marker), or IL-17F (Th17 marker) using real-time PCR on the ViiA7 thermocycler with predesigned TaqMan Assay-on-Demand gene expression primer/probe sets (Applied Biosystems). Gene expression was normalized to 18S and expressed as ΔCt values, with ΔCt = Ctgene − Ct18S or expressed as relative mRNA level of specific gene expression as obtained using the 2−ΔCt method. |
| Concentrations | 10, 1, 0.1 or 0 μM |
| Incubation time | 5 days |
| Animal Experiment | |
|---|---|
| Animal models | therapeutic rat CIA model |
| Formulation | 0.05 M acetic acid |
| Dosages | 50 mg/kg twice daily for 14 d |
| Administration | oral |
| Molecular Weight | 425.5 |
| Formula | C21H23N5O3S |
| CAS Number | 1206161-97-8 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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