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KTC1101

Chemical Structure : KTC1101

CAS No.: 2764833-47-6

KTC1101 (KTC-1101)

Catalog No.: PC-22175Not For Human Use, Lab Use Only.

KTC1101 is a potent, selective pan-PI3K inhibitor with IC50 of 3.72 nM for PI3Kα, 36.29 nM for PI3Kβ, 1.22 nM for PI3Kδ, and 17.09 nM for PI3Kγ.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

KTC1101 is a potent, selective pan-PI3K inhibitor with IC50 of 3.72 nM for PI3Kα, 36.29 nM for PI3Kβ, 1.22 nM for PI3Kδ, and 17.09 nM for PI3Kγ.
KTC1101 (1 uM) robustly inhibits all four PI3K targets with an inhibition rate greater than 90%, while maintaining an inhibition rate of less than 50% for a comprehensive panel of 50 kinases.
KTC1101 demonstrates broad-spectrum anti-proliferative activity across diverse tumor cell lines in vitro, displays superior inhibitory performance in TMD8 cells, when compared to both Copanlisib and ZSTK474.
KTC1101 exhibitsa mean GI50 value of 23.4 nM across a panel of 39 human tumor cell lines, significantly lower than that of ZSTK474 (320 nM) and Copanlisib (134 nM).
KTC1101 demonstrates favorable pharmacological properties and pronounced anti-tumor activity in mice.
KTC1101 has potential to activate tumor immunity through tumor-cell-intrinsic effects and direct T-cell modulation, synergizes with anti-PD-1 therapy.

Physicochemical Properties

M.Wt 476.49
Formula C21H26F2N8O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(difluoromethyl)-4-methoxy-1-(4-morpholino-6-(1,4-oxazepan-4-yl)-1,3,5-triazin-2-yl)-1H-benzo[d]imidazol-6-amine

References

1. Peng X, et al. Mol Cancer. 2024 Mar 14;23(1):54.

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