p18

Description: P-18 (P18) is a novel and potent inhibitor of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 (PD-1/PD-L1) Interaction with IC50 of 9 nM in homogeneous time-resolved fluorescence (HTRF) binding assays. P18 promoted HepG2 cell death dose dependently in a HepG2/PD-L1 and Jurkat/PD-1 coculture cell model. Further, P18 demonstrated significantly higher water

solubility (17.61 mg/mL) and improved pharmacokinetics (e.g., t1/2 of ?20 h and oral bioavailability of 12%) than the previous analogues. Moreover, P18 was highly effective in suppressing tumor growth in an immune checkpoint humanized mouse model without apparent toxicity.

References: J Med Chem. 2020 Dec 24; 63(24):15946-15959.