PD-1
| 中文名称 | PD-1 |
|---|---|
| 中文同义词 | (2S)-1-[[2,6-二甲氧基-4-[(2-甲基[1,1'-联苯]-3-基)甲氧基]苯基]甲基]-2-哌啶羧酸;(S)-1-(2,6-二甲氧基-4-((2-甲基-[1,1'-联苯]-3-基)甲氧基)苄基)哌啶-2-甲酸;PD-L1 抑制剂1;化合物PD-1/PD-L1 INHIBITOR 1;PD-1/PD-L1抑制剂杂质8(BMS 1);PD-1 / PD-L1抑制剂1;(S)-1-(2,6-二甲氧基-4-((2-甲基-[1,1'-联苯]-3-基)甲氧基)苄基)哌啶-2-甲酸 |
| 英文名称 | 2-Piperidinecarboxylic acid, 1-[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-, (2S)- |
| 英文同义词 | 2-Piperidinecarboxylic acid, 1-[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-, (2S)-;PD1-PDL1 inhibitor 1;PD-1PD-L1 inhibitor;(2S)-1-[[2,6-Dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-piperidinecarboxylic acid;avelumab/PD-L1;T3655;(2S)-1-{2,6-Dimethoxy-4-[(2-methyl-3-biphenylyl)methoxy]benzyl}-2-piperidinecarboxylic acid;PD1-PDL1 inhibitor 1 (PD1-PDL1-IN1) |
| CAS号 | 1675201-83-8 |
| 分子式 | C29H33NO5 |
| 分子量 | 475.58 |
| EINECS号 | |
| 相关类别 | 其他生化试剂;抑制剂;原料药及中间体 |
| Mol文件 | 1675201-83-8.mol |
| 结构式 |  |
PD-1 性质
| 沸点 | 630.2±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.182±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 可溶于 DMSO（高达至少 25 mg/ml）或乙醇（高达 20 mg/ml） |
| 酸度系数(pKa) | 2.34±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色 |
| 稳定性 | 自购买之日起，稳定期为 1 年。 其DMSO 或乙醇溶液可在 -20°C 下保存长达 3 个月。 |
BMS-1 (PD-1/PD-L1 inhibitor 1, PD1-PDL1-IN1)是一种PD-1/PD-L1相互作用的小分子化合物抑制剂，IC50为6 nM。
| Target | Value |
|
PD-1/PD-L1 interaction
(Cell-free assay) | 0.006 μM |
Since PD-1 mediated the exhaustion of natural killer (NK) cell by binding to its ligand PD-L1, BMS-1 (PD-1/PD-L1 inhibitor 1) (1 μM, 3 days) is used to disturb the interaction between PD-1 and PD-L1. Dexamethasone induced increase of PD-1 expression and decrease of cytotoxicity of the co-cultured NK92 cells are reversed by BMS-1. BMS-1, a small-molecule immune checkpoint inhibitor of PD-1/PD-L1, can be used as a therapeutic strategy for tumor immunotherapy.
Cell Cytotoxicity Assay
| Cell Line: | NK cells and HepG2 cells |
| Concentration: | 1 μM |
| Incubation Time: | 3 days |
| Result: | Disturbed the interaction between PD-1 and PD-L1. |
BMS-1 (500 μg/mL; 100 μL; i.p.) significantly slows down tumor growth and prolongs the survival rates in BALB/c mice.
| Animal Model: | BALB/c mice |
| Dosage: | 500 μg/mL; 100 μL |
| Administration: | I.p. |
| Result: | Administration significantly slowed down tumor growth and prolonged the survival rates. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-19991 | PD-1 BMS-1 | 1675201-83-8 | 5mg | 1200元 |
| 2024/01/25 | HY-19991 | PD-1 BMS-1 | 1675201-83-8 | 10mM * 1mLin DMSO | 1320元 |