BMS-202

BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC₅₀ of 18 nM and a K_D of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity^[1][2]. IC50 & Target: IC50: 18 nM (PD-1/PD-L1)^[1]
KD: 8 μM (PD-1/PD-L1)^[1] In Vitro: BMS-202 (0-100 μM; 4 days; SCC-3 or Jurkat cells) treatment inhibits the proliferation of strongly PD-L1-positive SCC-3 cells (IC₅₀ of 15 μM) and anti-CD3 antibody-activated Jurkat cells (IC₅₀ 10 μM) in vitro^[2].
BMS-202 selectively induces thermal stabilization of PD-L1. BMS-202 induces dimerization of PD-L1 in solution.BMS-202 is located at the center of the homodimer filling a deep hydrophobic pocket contributing multiple additional interactions between the monomers. BMS-202 interacts with both PD-L1 molecules using hydrophobic surfaces physiologically involved in the PD-1/PD-L1 interaction^[1]. In Vivo: BMS-202 (20 mg/kg; intraperitoneal injection; daily; for 9 days; NOG-dKO mice) treatment shows a clear antitumor effect compared with the controls, in humanized MHC- dKO NOG mice^[2].