Pilaralisib

Pilaralisib (CAS No.: 934526-89-3) is a rationally designed synthetic small-molecule, reversible, and selective class I phosphoinositide 3-kinase (PI3K) inhibitor, also known as XL147/SAR245408, primarily used as a signal transduction research tool in oncology and immunology models; it preferentially acts on the p110α, p110δ, and p110γ isoforms, with relatively lower activity against p110β, and attenuates downstream AKT/mTOR pathway signaling by inhibiting the generation of phosphatidylinositol trisphosphate, enabling selective pathway modulation in biochemical and cellular systems; in ex vivo biochemical assays, it typically shows inhibitory activity in the nanomolar to low-nanomolar range, while in cellular models, pathway inhibition and effects on cell proliferation are more commonly observed at low to mid-micromolar levels; inhibition of class III PI3K (such as Vps34), DNA-dependent protein kinase, and mTOR generally appears only at higher exposure levels, reflecting a relatively favorable selectivity profile; typical research applications include target validation, pathway mapping and functional dependency assessment, combination-mechanism studies with receptor tyrosine kinase or HER family pathway modulators, and confirmation of target occupancy in xenograft animal models by monitoring pharmacodynamic readouts such as reduced phosphorylation of downstream effector proteins; this compound is suitable for mechanistic elucidation and early-stage drug discovery screening, and the concentration or dose used in experiments should be determined according to the specific experimental design and research objectives, and is limited to laboratory research use only.