BMS-1166 HCl Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO: soluble

form 

A solid

color 

White to off-white

InChIKey

HYWQPFPFYSOTHD-PVIANJOKNA-N

SMILES

C(N1C[C@H](O)C[C@@H]1C(=O)O)C1C=C(Cl)C(OCC2C=CC=C(C3=CC=C4OCCOC4=C3)C=2C)=CC=1OCC1C=CC=C(C#N)C=1.Cl |&1:3,6,r|

BMS-1166 HCl Usage And Synthesis

Description

BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor. BMS-1166 binds to human PD-L1 and blocks its interaction with PD-1. BMS-1166 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. Moreover, BMS-1166 was effective in attenuating the inhibitory effect of the cell surface-associated PD-L1.

Uses

BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation[1][2].

target

BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor.

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. DOI:10.1021/acs.jmedchem.7b00293
[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. DOI:10.18632/oncotarget.20050

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