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説明

The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival. CAL-101 is a cell permeable inhibitor of the PI3K catalytic subunit p110δ (IC50 = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC50s = 820, 565, and 89 nM for p110α, β, and γ, respectively). At 1 μM it can block constitutive PI3K signaling in malignant B-cell lines and primary patient tumor cells, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase, and apoptosis. It has also been shown to inhibit the chemotaxis of chronic lymphocytic leukemia cells and to downregulate the secretion of chemokines triggered by B-cell receptor signaling.