PI3Kα Inhibitor

Izorlisib (CH5132799) methanesulfonate is an orally active, selective Class I PI3K inhibitor with an IC₅₀ value of 14 nM against PI3Kα. Izorlisib methanesulfonate specifically inhibits Class I PI3K (particularly PI3Kα and its mutants) and blocks the PI3K/Akt/mTOR pathway; this leads to cell cycle arrest at the G1 phase and apoptosis without triggering feedback activation of Akt by competitively binding to the ATP-binding site of PI3K. Izorlisib methanesulfonate can be used in research on cancers harboring PIK3CA mutations or PTEN loss (such as breast, ovarian, prostate, and endometrial cancers).

AM-0687 is a selective inhibitor for PI3Kδ with an IC₅₀ of 2.9 nM. AM-0687 decreases the levels of IgG and IgM specific antibodies, inhibits the anti-IgM/CD40L-induced proliferation of human B cell (IC₅₀=0.8 nM) and the phosphorylation of AKT (IC₅₀=0.7 nM), and exhibits anti-inflammatory efficacy.

SPR519 is a selective, orally active dual PI3Kα/mTOR kinase inhibitor, with an IC₅₀ of 0.03 μM against PI3Kα and an IC₅₀ of 0.01 μM against mTOR. SPR519 exhibits anticancer effects in ovarian cancer and colon cancer xenograft models. SPR519 can be used for the research of solid tumors (ovarian cancer, colon cancer).

PIK-C98 is a potent and selective PI3K inhibitor, with IC₅₀s of 0.59, 1.64, 3.65, and 0.74 μM for α, β, δ, and γ isoforms, respectively. PIK-C98 inhibits all class I PI3Ks but has no effects on AKT or mTOR activity. PIK-C98 interferes with the ATP-binding pockets of PI3Ks by forming H-bonds and arene-H interactions with specific amino acid residues. PIK-C98 induces apoptosis by inhibiting PI3K. PIK-C98 can be used for the research of multiple myeloma.

Bimiralisib hydrochloride (PQR309 hydrochloride) is an orally active, blood-brain barrier-penetrant PI3K/mTOR inhibitor with in vitro antiproliferative activity and in vivo antitumor activity. Bimiralisib hydrochloride induces G1 cell cycle arrest, apoptosis and cell death in cancer cells, while inhibiting cancer cell proliferation, migration, invasion, colony formation and spheroid generation. Bimiralisib hydrochloride upregulates the expression of E2F4. The combination of Bimiralisib hydrochloride with venetoclax enhances therapeutic efficacy in acute myeloid leukemia models. Bimiralisib hydrochloride can be used in cancer-related research.

mTOR inhibitor-10 (Compound 9c) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC₅₀ of 0.7 and 825 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC₅₀ of 87 nM.

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC₅₀s of 1.3 and 6.1 nM, respectively.