pqr 309

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.