KTC1101 

KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response^[1].

KTC1101 (0.1-50000 nM, 48 h) can dose-dependently induce cell cycle stagnation in G1 phase in all tested cell lines (PC3, TMD8, HSC2, HSC4, and CAL33 cells). KTC1101 has anti-proliferative activity, with the IC₅₀ ranging from 20 nM to 130 nM, but has no significant promotion of apoptosis^[1].
KTC1101 (0.1-1000 nM, 1 h) exhibits significant inhibitory activity against all PI3K isoforms in the Adapta kinase assay. The IC₅₀ values of KTC1101 for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ are 3.72 nM, 36.29 nM, 1.22 nM and 17.09 nM respectively^[1].
KTC1101 (0-125 nM, 48 h) effectively inhibits the PI3K signaling pathway in WB experiments, reduces the phosphorylation of PI3K downstream effectors AKT and mTOR^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KTC1101 (0-125 mg/kg/day for 14 days, p.o.) can arrest tumor growth in mice with human tumor xenografts and show no signs of recurrence^[1].

Pharmacokinetic Analysis in tumor xenograft mouse model^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

476.48

C₂₁H₂₆F₂N₈O₃

2764833-47-6

FC(F)C1=NC2=C(OC)C=C(N)C=C2N1C3=NC(N4CCOCCC4)=NC(N5CCOCC5)=N3

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• [1]. Peng X, et al. A novel pan-PI3K inhibitor KTC1101 synergizes with anti-PD-1 therapy by targeting tumor suppression and immune activation. Mol Cancer. 2024 Mar 14;23(1):54.  [Content Brief]