pi3kα-h1047r

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

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.

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.

PI3Kα-IN-23 (Compound 9) is an inhibitor of PI3Ka H1047R.

PI3Kα-IN-29 is an efficacious, orally bioavailable, and selective PI3Kα inhibitor with an IC50 value of 2.5 nM. It demonstrates over 400-fold selectivity against PI3Kβ/δ/γ/mTOR. This compound selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses the PI3K/AKT/mTOR signaling pathway, induces G1 phase arrest, and inhibits cell migration. Additionally, it impedes tumor growth in T47 mouse models and is applicable for breast cancer research.

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.

PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].

PKI-179 hydrochloride is a potent and orally available dual PI3K/mTOR inhibitor. Its IC₅₀ values against PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR are 8 nM, 24 nM, 74 nM, 77 nM and 0.42 nM respectively. It also exerts inhibitory activity against E545K and H1047R mutants with IC₅₀ values of 14 nM and 11 nM, and exhibits significant antitumor effects in in vivo models.

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).

PI3Kα-IN-22 (Compound 17) is a potent, selective, and orally active inhibitor targeting the PI3Kα H1047R mutation, exhibiting an IC 50 of 1 nM in the pAKT T47D AlphaLISA assay. It has demonstrated the ability to induce tumor regressions in the HCC1954 tumor model in mice [1].