CNX-1351 (CNX1351; CNX 1351) is a novel, potent, covalent and selective inhibitor of PI3Kα with anticancer activity. It inhibits PI3Kα with an IC50 of 6.8 nM. CNX-1351 acts by covalently modifying PI3Kα on cysteine 862 (C862), an amino acid unique
to the α isoform, and that PI3Kβ, -γ, and -δ are not covalently
modified. It is able to potently (EC(50) < 100 nM) and specifically
inhibit signaling in PI3Kα-dependent cancer cell lines, and this leads
to a potent antiproliferative effect (GI(50) < 100 nM).
纯度:≥98%
CAS:1276105-89-5