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BMS-202

CAS No. : 1675203-84-5

產(chǎn)品活性：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.

研究領(lǐng)域：Immunology/Inflammation  |  Apoptosis

作用靶點(diǎn)：PD-1/PD-L1  |  Apoptosis

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.
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.

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.

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