PI3Kδ-IN-11

PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

PI3Kδ:27.5 nM (IC50)

PI3Kδ-IN-11 (compound 15c) (0-10 μM; 48 hours) inhibits Raji and Ramos with IC50s of 8.5 μM and 5.4 μM, respectively[1]. PI3Kδ-IN-11 (0.2-15 μM; 0-48 hours) dampens the proliferation of Raji cells in a dose- and time-dependent manner[1]. PI3Kδ-IN-11 (5 μM; 24 hours) triggers 10.78% apoptosis of cells[1]. PI3Kδ-IN-11 (1-1000 nM; 24 hours) dose-dependently reduces the phosphorylation of Akt (S473)[1]. Cell Viability Assay Cell Line: Raji and Ramos[1] Concentration: 0-10 μM Incubation Time: 48 hours Result: Inhibited Raji and Ramos with IC50s of 8.5 μM and 5.4 μM, respectively. Cell Proliferation Assay Cell Line: Raji[1] Concentration: 0.2, 1, 4, 8, 10 and 15 μM Incubation Time: 0, 12, 24, 36, 48 hours Result: Dampened the proliferation of Raji cells in a dose- and time-dependent manner. Apoptosis Analysis Cell Line: Raji[1] Concentration: 5 μM Incubation Time: 24 hours Result: Triggered 10.78% apoptosis of cells. Western Blot Analysis Cell Line: Raji[1] Concentration: 1, 10, 100, 500 and 1000 nM Incubation Time: 24 hours Result: Dose-dependently reduced the phosphorylation of Akt (S473), illustrating that the activity of PI3K/Akt pathway was efficiently blocked.

[1]. Teng Y, Li X, Ren S, et al. Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity. Eur J Med Chem. 2020;208:112865.