| Identification | Back Directory | [Name]
PD-1/PD-L1-IN1 | [CAS]
1818314-88-3 | [Synonyms]
PD-1/PD-L1-IN1
PD-1/PD-L1-IN1 BMS-1166
BMS-1166 (PD-1/PD-L1-IN1)
BMS-1166 (Synonyms: PD-1/PD-L1-IN1)
D-Proline, 1-[[5-chloro-2-[(3-cyanophenyl)methoxy]-4-[[3-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-methylphenyl]methoxy]phenyl]methyl]-4-hydroxy-, (4R)- | [Molecular Formula]
C36H33ClN2O7 | [MDL Number]
MFCD31746874 | [MOL File]
1818314-88-3.mol | [Molecular Weight]
641.11 |
| Chemical Properties | Back Directory | [Boiling point ]
817.5±65.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml | [form ]
A crystalline solid | [pka]
2.03±0.40(Predicted) | [color ]
White to off-white | [InChIKey]
QBXVXKRWOVBUDB-GRKNLSHJSA-N | [SMILES]
C(O)(=O)[C@H]1C[C@@H](O)CN1CC1=CC(Cl)=C(OCC2=CC=CC(C3=CC=C4OCCOC4=C3)=C2C)C=C1OCC1=CC=CC(C#N)=C1 |
| Hazard Information | Back Directory | [Uses]
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation[1][2]. | [Biological Activity]
BMS-1166 is a novel and potent inhibitor of PD-1/PD-L1 interaction with IC50 of 1.4 nM. | [in vitro]
BMS-1166 had low toxicity to the tested cell lines and prevented the interaction of soluble PD-L1 with PD-1 receptors expressed on the cell surface. It attenuates the inhibitory effect of PD-L1 on T cell receptor-mediated T lymphocyte activation. | [target]
| Target | Value | PD-1/PD-L1 interaction
() | 1.4 nM |
| [storage]
Store at -20°C | [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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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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