BKM120 is a potent and highly specific pan-class I PI3K inhibitor. It exhibits 50-300nM activity for class I PI3Ks, including the most common p110? mutants. It is less potent against class III and class IV PI3Ks. In addition, it shows no significant inhibition against related kinases, including VPS34, mTOR, DNAPK and PI4K [1].

Abnormal activation of the PI3K-AKT-mTOR pathway is frequently observed in many types of cancer. Targeting the PI3K-AKT-mTOR pathway could arrest tumor growth and induce cell death in cancers. KM120 alone or in combination with other agents induced apoptosis and inhibit proliferation (IC50 of 0.15-0.7nM) in a broad range of PI3K deregulated tumor cells. Inhibition of PI3K by BMK120 together with STAT3 blockade induces apoptosis synergistically in gastric cancer cells harboring mutated KRAS but not in KRAS wild-type cells. BKM120 treatment results in significantly reduced tumor volume and prolonged survival in mouse models [1-4]. BKM120 is currently being investigated in Phase I and II clinical trials in advanced solid tumor patients as a single agent as well as in combination with other agents.

BKM120 is a potent and highly specific pan-class I PI3K inhibitor. It exhibits 50-300nM activity for class I PI3Ks, including the most common p110? mutants. It is less potent against class III and class IV PI3Ks. In addition, it shows no significant inhibition against related kinases, including VPS34, mTOR, DNAPK and PI4K [1].

Abnormal activation of the PI3K-AKT-mTOR pathway is frequently observed in many types of cancer. Targeting the PI3K-AKT-mTOR pathway could arrest tumor growth and induce cell death in cancers. KM120 alone or in combination with other agents induced apoptosis and inhibit proliferation (IC50 of 0.15-0.7nM) in a broad range of PI3K deregulated tumor cells. Inhibition of PI3K by BMK120 together with STAT3 blockade induces apoptosis synergistically in gastric cancer cells harboring mutated KRAS but not in KRAS wild-type cells. BKM120 treatment results in significantly reduced tumor volume and prolonged survival in mouse models [1-4]. BKM120 is currently being investigated in Phase I and II clinical trials in advanced solid tumor patients as a single agent as well as in combination with other agents.