产品描述:
CNX-1351 is a covalent inhibitor of PI3Kα (IC50 = 6.8 nM).{56002} It is selective for PI3Kα over PI3Kβ, -γ, and -δ (IC50s = 166, 240.3, and 3,020 nM, respectively), as well as PI3KC2A, PI3KC, PI4Kα, PI4Kβ, SPHK1, and SPHK2 (IC50s = >1 µM for all). CNX-1351 (500 nM) inhibits phosphorylation of Akt in SKOV3 cells. It inhibits the growth of SKOV3 and MCF-7 cancer cells (GI50s = 77.6 and 54.7 nM, respectively). CNX-1351 (100 mg/kg) inhibits Akt phosphorylation in mouse spleen.