SYN-1230 | CAS 1217486-61-7
Alpelisib (BYL719) is a selective PI3Kα inhibitor with IC50 of 5 nM. It has minimal effect on PI3K isoforms. Alpelisib exhibits favourable pharmacokinetics and excellent oral bioavailability in animal models. In xenografts using nude mice, it showed dose-dependent effect of tumour inhibition. In a phase Ib study, it showed synergistic anti-tumor activity with endocrine therapy against ER+/PIK3CA mutated breast cancer cells.