SN32976

SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC₅₀s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects^[1]. In Vitro:SN32976 (1-100 nM; for 1 h) inhibits both Thr308 and Ser473 pAKT expression in U-87 MG cells at concentrations as low as 10 nM^[1].
The cell lines are PTEN null (U-87 MG, PC3, NZM34), H1047R PIK3CA mutant (HCT116, NZM40), E545K PIK3CA mutant (NCI-H460, MCF7) and PIK3CA amplified (FaDu). SN32976 potently inhibits cell proliferation in all cell lines, with EC₅₀ values ranging from 18.5 nM in NCI-H460 cells to 1787 nM in NZM34 cells^[1]. In Vivo:SN32976 (37.5-75 mg/kg; po; daily; for 21 days) inhibits tumor growth in U-87 MG tumor xenograft models^[1].