Pilaralisib (XL147, SAR245408) is a potent and highly selective, orally active class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively.
Pilaralisib (XL147, SAR245408) shows broad kinase selectivity profiling of >130 protein kinases.
Pilaralisib (XL147, SAR245408) inhibits the formation of PIP3 in the membrane, and inhibits phosphorylation of AKT, p70S6K, and S6 in multiple tumor cell lines with diverse genetic alterations affecting the PI3K pathway in cellular assays.
Pilaralisib (XL147, SAR245408) inhibits proliferation with a wide range of potencie in a panel of tumor cell lines.
Pilaralisib (XL147, SAR245408) induces dose-dependent inhibition of phosphorylation of AKT, p70S6K, and S6 with a duration of action of at least 24 hours in mouse xenograft models, causes significant tumor growth inhibition in multiple human xenograft models in nude mice.