PF-4989216 是一种有效的选择性PI3K抑制剂，对p110α，p110β，p110γ，p110δ，和 VPS34的 IC50 分别为 2 nM，142 nM，65 nM，1 nM，和 110 nM。 Information PF-4989216 is a potent and selectivePI3Kinhibitor withIC50of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. Targets p110δ (Cell-free assay); p110α (Cell-free assay); p110γ (Cell-free assay) 1 nM; 2 nM; 65 nM In vitro PF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis. In vivo In SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity. Cell Research(from reference) Cell lines：NCI-H69, NCI-H1048, NCI-H1436, NCI-H82, NCI-H254, NCI-H526, NCI-H1963, NCI-H146, NCI-H841, Lu99A, Lu134B, and Lu134A cells. Concentrations：~10 μM Incubation Time：72 hours