1033739-92-2

GNE-490 is a highly selective pan-PI3K inhibitor, demonstrating selectivity over mTOR.

GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for ?PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model[1].

PI3Kα: 3.5 nM (IC₅₀); PI3Kβ: 25 nM (IC₅₀); PI3Kδ: 5.2 nM (IC₅₀); PI3Kγ: 15 nM (IC₅₀); mTOR: 750 nM (IC₅₀)

[1] Daniel P Sutherlin, et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem. 2010 Feb 11;53(3):1086-97. DOI:10.1021/jm901284w