生物活性：
BBO-10203 is a potent inhibitor of PI3Kα and KRASG12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRASG12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer.

体内活性：
BBO-10203 (口服；每日一次) 显著抑制异种移植模型中的肿瘤生长。

体外活性：
BBO-10203 (300 nM；24 小时) 降低 NCI-H2122 中的细胞增殖和 pAKT 磷酸化。 BBO-10203 (24 小时) 降低 MCF7 中的细胞增殖。 BBO-10203 增加 NSCLC 中的凋亡。