Catalog No.: PC-25282Not For Human Use, Lab Use Only.
CNX-1351 (CNX1351) is a potent, isoform-selective and covalent inhibitor of PI3Kα with IC50 of 6.8 nM, covalently modifies PI3Kα on cysteine 862 (C862).
CNX-1351 (CNX1351) is a potent, isoform-selective and covalent inhibitor of PI3Kα with IC50 of 6.8 nM, covalently modifies PI3Kα on cysteine 862 (C862). CNX-1351 does not covalently modifies PI3Kβ, -γ, and -δ and shows no inhibitory activities. CNX-1351 inhibits PI3K signaling in SKOV3 cells with EC50 of 10-100 nM in SKOV3 cells, irreversibly inhibits p-AktSer473. CNX-1351 inhibits cell growth of cance cell with PIK3CA activating mutations, SKOV3 ovarian cancer cells (H1047R) and MCF-7 breast cancer cells (E545K), with IC50 of 77.6 and 54.7 nM respectively. CNX-1351 (100 mg/kg ip) inhibits p-AktSer473 in mouse spleens and binds to PI3Kα in vivo.
