BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.
IC50&Target
IC50: 18 nM (PD-1/PD-L1)
KD: 8 μM (PD-1/PD-L1)
体外研究
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.
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.
Cell Proliferation Assay
Cell Line:
SCC-3 or Jurkat cells
Concentration:
0-100 μM
Incubation Time:
4 days
Result:
Inhibited 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.
体内研究
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.
Animal Model:
NOG-dKO mice (8-week-old) injected with SCC-3 cells
Dosage:
20 mg/kg
Administration:
Intraperitoneal injection; daily; for 9 days
Result:
Showed 41% growth inhibitory activity against humanized mouse-transplanted human lymphoma SCC-3 cells.
分子式
C25H29N3O3
分子量
419.52
CAS号
1675203-84-5
运输条件
Room temperature in continental US; may vary elsewhere.