Duvelisib R enantiomer is the R-isomer of Duvelisib (formerly known as IPI-145 and INK1197, trade name: Copiktra) which is an isoquinolinone derivative and a novel potent, oral and selective small-molecule phosphoinositide-3 kinases (PI3K) inhibitor that selectively and potently inhibits two PI3K isoforms, PI3K-δ and PI3K-γ, with half maximal inhibition concentration IC50 of 2.5 nM and 27 nM respectively. FDA approved duvelisib in September 2018 to treat small lymphocytic lymphoma, follicular lymphoma, and chronic lymphocytic leukemia that has relapsed or is resistant to treatment. Despite having a preference for PI3K-δ and PI3K-γ, IPI-145 also inhibits PI3K-α and PI3K-β to a lesser extent, with IC50 values of 1602 nM and 85 nM, respectively. Phosphoinositide-3-kinase (PI3K) is an enzyme group, known to regulate key survival pathways in acute myeloid leukaemia (AML). It produces phosphatidylinositol-3,4,5-triphosphate, which offers a membrane docking site for protein kinaseB activation. There are four isoforms of the p110 catalytic subunit of PI3K:,, and. In contrast to the highly variable frequency of PI3Kγ expression, the PI3Kδ isoform is consistently expressed in AML cells. The roles of these individual catalytic enzymes have not been fully elucidated in AML, so the function of these two p110 subunits in human AML blast survival was investigated using the PI3K p110δ and p110γ targeted inhibitor IPI-145 (duvelisib) and specific p110δ and p110γ shRNA.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.