KTC1101 is an oral-active, pan-PI3K inhibitor targeting tumor cell proliferation and tumor microenvironment, with anti-proliferative and anti-tumor activity, reducing downstream AKT and mTOR phosphorylation.

PI3Kα:3.72 nM, PI3Kδ:1.22 nM, PI3Kβ:36.29 nM, PI3Kγ:17.09 nM

The IC50 values of KTC1101 for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ were 3.72 nM, 36.29 nM, 1.22 nM and 17.09 nM, respectively.
KTC1101 effectively inhibited the PI3K signaling pathway, and the phosphorylation of PI3K downstream effector AKT and mTOR was decreased. [1]

In mice, KTC1101 (100 mg/kg) has good oral effect, Tmax is 0.67 h, Cmax is 1.66 μg/mL, AUC0-t is 9.33 μg/mL*h.
KTC1101 (100 mg/kg) showed favorable tumor inhibition in mice in four tumor models tested (PC3, CAL33, and HSC2). [1]