| E1852 |
RLY-2608 |
RLY‑2608 (zovegalisib) is an oral, first‑in‑class allosteric, pan‑mutant‑selective inhibitor of PI3Kα that preferentially targets oncogenic PIK3CA mutants, retaining antitumor activity while reducing PI3Kα‑related metabolic toxicities. |
| 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). |