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BMS-1166 hydrochloride

Names

[ CAS No. ]:
2113650-05-6

[ Name ]:
BMS-1166 hydrochloride

Biological Activity

[Description]:

BMS-1166 hydrochloride is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Immunology/Inflammation >> PD-1/PD-L1
Research Areas >> Inflammation/Immunology

[Target]

IC50: 1.4 nM (PD-1/PD-L1 interaction)[1].


[In Vitro]

BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM in a homogenous time-resolved fluorescence binding assay[1]. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation. BMS-1166 dose dependently abolishes the inhibition of ECs stimulation by sPD-L1[2].

[References]

[1]. Guzik K, et al. Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1. J Med Chem. 2017 Jul 13;60(13):5857-5867.

[2]. Skalniak L, et al. Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells. Oncotarget. 2017 Aug 7;8(42):72167-72181.

Chemical & Physical Properties

[ Molecular Formula ]:
C36H34Cl2N2O7

[ Molecular Weight ]:
677.57

Related Compounds