A66 inhibits the oncogenic forms of p110α such as E545K H1047R with IC50 of 30 nM and 43 nM, respectively. A66 displays >100-fold selectivity for p110α over other class-I PI3K isoforms. Among the class-II PI3Ks, class-III PI3Ks, and PI4Ks, A66 only exhibits limited cross-reactivity with the class-II PI3K PI3K-C2β and the PI4Kβ isoform of PI4K with IC50 of 462 nM and 236 nM, respectively. A66 exhibits no inhibitory activity against other lipid kinases or the related kinases DNA-PK and mTOR. A66 treatment at 0.7 μM induces a 75-80% reduction in focus formation by the highly transforming p85α iSH2 mutants KS459delN, DKRMN-S560del, and K379E, and reduces the phosphorylation of Akt on T308 by all p85 mutants.
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