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.

mTOR:12 nM(Kd), PI3Kγ:25 nM(Kd), PI3Kα:1.5 nM(Kd), PI3Kβ:11 nM(Kd), PI3Kδ:25 nM(Kd), PI3Kα (H1047R):36 nM, PI3Kα (E542K):136 nM, DNA-PK:8567 nM, PI3Kα (E542K):63 nM, VPS34:6486 nM