GDC-0032

GDC-0032 (Taselisib) is a cell permeable, orally bioavailable, and next-generation β isoform-sparing pan PI3K inhibitor. Embedded with unique features, GDC-0032 is a much more upgraded version of GDC-0941 (Pictilisib) in most pharmacological parameters. It potently and selectively inhibits PI3Kα /δ /γ isoforms with IC50 values of 0.29 nM/0.12 nM/0.97nM, with reduced inhibitory potency against PI3Kβ (IC50 >8 nM, >30 fold less potent relative to the PI3Kα isoform). This selectivity and isoform-biased profile has allowed for greater efficacy in vivo at the maximum tolerated dose relative to a pan inhibitor in representative PI3Kα (PIK3CA) mutant xenografts, and noticeably it preferentially inhibited PIK3CA mutant cells relative to cells with wild-type PI3K. It is currently in clinical evaluation.

Soluble in DMSO