Product Name: GLPG-0634 (Filgtinib)
GLPG-0634 Chemical Structure
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GLPG0634 is an orally-available, selective inhibitor of JAK1 (Janus kinase 1) being developed by Galapagos for the treatment of rheumatoid arthritis and potentially other inflammatory diseases.
GLPG-0634 is a selective covalent Inhibitor of PI3Kα. GLPG-0634 was tested against all four of the class I PI3K enzymes α, β, γ, and δ. In an end point assay, GLPG-0634 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, and δ. GLPG-0634 inhibit PI3Kα signaling in cells and shows prolonged inhibition consistent with a covalent mechanism of Action. GLPG-0634 inhibits growth of cells dependent on PI3Kα. GLPG-0634 also inhibits PI3Kα signaling in vivo and bonds to p110α.
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