ppkb

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

PI3K-IN-2 are orally active PI3Kβ/δ inhibitors with IC50 values of 7.1 nM, 8.6 nM, and higher selectivity than PI3Kσ (IC50: 13 nM) and PI3Kγ (IC50: 190 nM), respectively.