BMS-202BMS-202
MedChemExpress (MCE)
HY-19745
1675203-84-5
99.48%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Room temperature in continental US
may vary elsewhere.
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.
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].
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].
IC50: 18 nM (PD-1/PD-L1)[1] KD: 8 μM (PD-1/PD-L1)[1] Cellular Effect Cell Line Type Value Description References
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[1]. Zak KM, et al. Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1). Oncotarget. 2016 May 24
7(21):30323-35. [Content Brief]
[2]. Ashizawa T, et al. Antitumor activity of the PD-1/PD-L1 binding inhibitor BMS-202 in the humanized MHC-double knockout NOG mouse. Biomed Res. 2019
40(6):243-250. [Content Brief]