PD-1/PD-L1-IN-24

PD-1/PD-L1-IN-24 is a highly potent PD-1/PD-L1 inhibitor with IC50 value of 1.57 nM. PD-1/PD-L1-IN-24 can restore T-cell function at the cellular level by significantly elevating the IFN-γ level. PD-1/PD-L1-IN-24 has low toxicity on the PBMCs[1].

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> PD-1/PD-L1

IC50: 1.57 nM (PD-1/PD-L1)[1]

PD-1/PD-L1-IN-24 (compound 39) (0-10 μM; 6 hours) significantly releases PD-L1-mediated inhibition of PD-1-expressing Jurkat T cells at the concentration of 10 μM[1]. PD-1/PD-L1-IN-24 (0.003-20 μM; 72 hours) exhibits no significant toxicity at concentrations ranging from 0.003 to 2.22 μM, and the IC50 is 12.42 μM[1]. PD-1/PD-L1-IN-24 (0.082, 0.247, 0.741 and 2.222 μM; 72 hours) significantly elevates the secretion of IFN-γ with a dose-dependent manner in T cell-tumor co-culture cells[1]. Cell Cytotoxicity Assay Cell Line: PBMC[1] Concentration: 0.003, 0.0091, 0.027, 0.082, 0.247, 0.741, 2.222, 6.67 and 20 μM Incubation Time: 72 hours Result: No significant toxicity was observed at concentrations ranging from 0.003 to 2.22 μM, and the IC50 was 12.42 μM.

[1]. Wang Y, Kun Huang, Gao Y, et al. Discovery of quinazoline derivatives as novel small-molecule inhibitors targeting the programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) interaction. Eur J Med Chem. 2022;229:113998.