BMS-202 是一种有效的非肽类 PD-1/PD-L 复合物抑制剂，其 IC₅₀ 为 18 nM，K_D 为 8 μM。BMS-202 与 PD-L1 直接结合并阻断人类 PD-1/PD-L 的相互作用。BMS-202 具有抗肿瘤活性。

BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC 50 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.

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IC50: 18 nM (PD-1/PD-L1)
KD: 8 μM (PD-1/PD-L1)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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Powder -20°C 3 years；4°C 2 years

[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.
[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.

In Vitro: DMSO : ≥ 100 mg/mL (238.37 mM)配制储备液