PD-L1 inhibitor 1
PD-L1 inhibitor 1 Basic information
- Product Name:
- PD-L1 inhibitor 1
- Synonyms:
-
- PD-L1 inhibitor 1
- PD1-PDL1 inhibitor 2
- N-[2-[[[2-Methoxy-6-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]-3-pyridinyl]methyl]amino]ethyl]acetamide
- BMS-202
- Acetamide, N-[2-[[[2-methoxy-6-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]-3-pyridinyl]methyl]amino]ethyl]-
- PD 1 inhibitor 2
- PD1 inhibitor 2
- PD-1 inhibitor 2
- CAS:
- 1675203-84-5
- MF:
- C25H29N3O3
- MW:
- 419.52
- Mol File:
- 1675203-84-5.mol
PD-L1 inhibitor 1 Chemical Properties
- Boiling point:
- 611.4±55.0 °C(Predicted)
- Density
- 1.133±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)
- form
- solid
- pka
- 16.06±0.46(Predicted)
- color
- White
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
PD-L1 inhibitor 1 Usage And Synthesis
Description
The programmed death-1/programmed death-ligand 1 (PD-1/PD-L1) interaction plays a dominant role in the suppression of T cell responses, especially in a tumor microenvironment, protecting tumor cells from lysis. PD-1/PD-L1 inhibitor 2 is reported to prevent the interaction of PD-L1 with PD-1 with an IC50 value of 18 nM.
Uses
BMS-202 is a Novel inhibitor of the PD-1/PD-L1 interaction by inducing PD-L1 dimerization through PD-1 interacting surface.
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[2].
| Animal Model: | NOG-dKO mice (8-week-old) injected with SCC-3 cells[2] |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 9 days |
| Result: | Showed 41% growth inhibitory activity against humanized mouse-transplanted human lymphoma SCC-3 cells. |
References
[1] KRZYSZTOF M ZAK. Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1).[J]. Oncotarget, 2016: 30323-30335. DOI:10.18632/oncotarget.8730
[2] KATARZYNA GUZIK. 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]. Journal of Medicinal Chemistry, 2017, 60 13: 5857-5867. DOI:10.1021/acs.jmedchem.7b00293
PD-L1 inhibitor 1Supplier
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