pi3kα-e542k

PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.

AZD-8835 is a mixed inhibitor of PI3Kα δ (IC50: 6.2 5.7 nM), also with selectivity against PI3Kβ γ (IC50: 431 90 nM).

ETP-46321 is an effective and orally bioavailable PI3Kα PI3Kδ inhibitor (Ki: 2.3 14.2 nM).

Gedatolisib (PF-05212384) is a highly effective dual inhibitor targeting the PI3Kα γ (IC50: 0.4 5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K mTOR signaling pathway.

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.