BYL719 is an inhibitor of phosphoinositide 3-kinase alpha (PI3Kalpha, IC50s = 4.6, 4, and 4.8 nM for wild-type, E545K mutant, and H1047R mutant PI3K, respectively). It is selective for PI3Kalpha over PI3Kbeta, PI3Kdelta, PI3Kgamma, and PI4Kbeta (IC50s = 1,156, 290, 250, and 581 nM, respectively), as well as VPS34,...

BLY719 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BYL719 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway.

Solid. Soluble in DMSO or DMF. Selective PI3Kalpha inhibitor with IC50 of 5nM. Has minimal effect on other PI3K isoforms. Exhibits favorable pharmacokinetics and excellent oral bioavailability in animal models. In xenografts using nude mice, it showed dose-dependent effects of tumour inhibition. In a phase Ib study,...

Description: Alpelisib (BYL-719) is a PI3Kalpha inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kbeta/gamma/delta with low activity (IC50=250/290/1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors. Target: PI3K. Smiles:...