Inavolisib CAS# 2060571-02-8

Inavolisib, also known as GDC-0077, is a potent and selective PI3K inhibitor. Inavolisib is an extraordinarily potent and selective PI3Kα inhibitor (IC₅₀ ≈ 0.038 nM), exhibiting over 300-fold selectivity versus other class I PI3K isoforms and >2000-fold over PIKK family members . In PIK3CA-mutant breast cancer cells (HCC1954, MCF7), it shows cellular EC₅₀ values of ~60 nM and ~30 nM, respectively . Mechanistically, it induces proteasome-dependent degradation of mutant p110α, suppresses downstream signaling (pAKT, pPRAS40), and triggers apoptosis, while wild-type cells are less affected. In vivo, oral dosing at or near the MTD produces dose-dependent tumor regressions, apoptosis, and downregulation of PI3K pathway biomarkers in multiple PIK3CA-mutant xenograft and PDX models