HomeNew PI3K Inhibitors

New PI3K Inhibitors

Catalog No. Product Name Information
E5872 BBO-10203 BBO-10203 inhibits PI3Kα and KRASG12C by covalently binding to Cys242 in the PI3Kα RAS-Binding Domain. It inhibits both GTP-bound and GDP-bound KRASG12C states, with IC50 and EC50 values of 0.031 nM and 0.02 nM respectively. This compound interferes with RAS-PI3Kα interaction, suppressing RAS-dependent PI3Kα activation. It decreases pERK levels, inhibits cell proliferation, and causes G1 phase arrest and apoptosis. BBO-10203 has potential applications in breast cancer, colorectal cancer, and non-small cell lung cancer research.
E1076 Linperlisib Linperlisibis a highly selective, orally bioavailable PI3Kδ inhibitor with an IC50 value of 6.4 nM, as disclosed in patent WO 2015055071 A1 (compound 10).
E1076 Linperlisib Linperlisibis a highly selective, orally bioavailable PI3Kδ inhibitor with an IC50 value of 6.4 nM, as disclosed in patent WO 2015055071 A1 (compound 10).
E1609 NVP-CLR457 NVP-CLR457 is an orally active, potent, and balanced inhibitor of pan-class I PI3K. NVP-CLR457 exhibits IC50 values of 12 ± 1.5 nM, 8.3 ± 1.0 nM, 8.3 ± 2.0 nM, 230 ± 31 nM, for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ. It shows a clear dose-dependent PK/PD/efficacy relationship and demonstrates antitumor activity.
E4605 Copanlisib dihydrochloride Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a selective and potent inhibitor of pan-class I PI3K. It significantly inhibits the catalytic activity of class I PI3K isoforms α, β, γ, and δ with IC50 of 0.5, 3.7, 6.4, and 0.7 nM, respectively. BAY 80-6946 exhibits potent antitumor activity in multiple cell-line–derived and patient-derived xenograft tumor models.
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