|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C21H23N5O3S |
|||
| Molecular Weight | 425.50 | CAS No. | 1206161-97-8 | |
| Solubility (25°C)* | In vitro | DMSO | 85 mg/mL (199.76 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
||||
Preparing Stock Solutions
Biological Activity
| Description | Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2. | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
||||||||
| In vitro | In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells. [1] | ||||||||
| In vivo | Following oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (∼100%). Filgotinib (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice. [1] Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon. [2] |
Protocol (from reference)
| Animal Study:[1] |
|
|---|
References
|
Customer Product Validation
-
Data from [Data independently produced by , , Arthritis Rheumatol, 2018, 70(12):2057-2066]
-
Data from [Data independently produced by , , Mol Cell Endocrinol, 2018, 472:26-39]
Selleck's Filgotinib (GLPG0634) has been cited by 48 publications
| Effects of an indole derivative on cell proliferation, transfection, and alternative splicing in production of lentiviral vectors by transient co-transfection [ PLoS One, 2024, 19(6):e0297817] | PubMed: 38833479 |
| Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44] | PubMed: 37726797 |
| JAK inhibitors differentially modulate B cell activation, maturation and function: A comparative analysis of five JAK inhibitors in an in-vitro B cell differentiation model and in patients with rheumatoid arthritis [ Front Immunol, 2023, 14:1087986] | PubMed: 36776828 |
| JAK inhibitors differentially modulate B cell activation, maturation and function: A comparative analysis of five JAK inhibitors in an in-vitro B cell differentiation model and in patients with rheumatoid arthritis [ Front Immunol, 2023, 14:1087986] | PubMed: 36776828 |
| JAK inhibitors differentially modulate B cell activation, maturation and function: A comparative analysis of five JAK inhibitors in an in-vitro B cell differentiation model and in patients with rheumatoid arthritis [ Front Immunol, 2023, 14:1087986] | PubMed: 36776828 |
| Sustained induction of IP-10 by MRP8/14 via the IFNβ-IRF7 axis in macrophages exaggerates lung injury in endotoxemic mice [ Burns Trauma, 2023, 11:tkad006] | PubMed: 37701855 |
| The protective effect of leukemia inhibitory factor on apoptosis of BMSCs induced by hypoxia and serum-deprivation [ Am J Transl Res, 2023, 15(6):4065-4078] | PubMed: 37434853 |
| Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44] | PubMed: 37726797 |
| Effects of Indole Derivative IDC16 on Cell Proliferation, Transfection, and Alternative Splicing in Production of Lentiviral Vectors by Transient Co-Transfection [ DigitalCommons, 2023, 10.26076/aa7d-bd6d] | PubMed: none |
| Tyrosine phosphorylation regulates RIPK1 activity to limit cell death and inflammation [ Nat Commun, 2022, 13(1):6603] | PubMed: 36329033 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.