中文名 | (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 | PD1-PDL1 inhibitor 1 |
别名 | 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 (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 |
英文别名 | PD-L1 T3655 avelumab PD-1PD-L1 inhibitor PD1-PDL1 inhibitor 1 (2S)-1-{2,6-Dimethoxy-4-[(2-methyl-3-biphenylyl)methoxy]benzyl}-2-piperidinecarboxylic acid (2S)-1-[[2,6-Dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-2-piperidinecarboxylic acid 2-Piperidinecarboxylic acid, 1-[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-, (2S)- |
CAS | 1675201-83-8 |
化学式 | C29H33NO5 |
分子量 | 475.576 |
密度 | 1.182±0.06 g/cm3(Predicted) |
沸点 | 630.2±55.0 °C(Predicted) |
溶解度 | 溶于DMSO (至少25毫克/毫升) 或乙醇 (高达20毫克/毫升) |
酸度系数 | 2.34±0.20(Predicted) |
存储条件 | -20℃ |
稳定性 | 从提供的购买之日起稳定1年。DMSO或乙醇中的溶液可以在-20 °C下储存长达3个月。 |
外观 | 固体 |
颜色 | White |
物化性质 | 生物活性 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。 |
靶点 | Target Value PD-1/PD-L1 interaction (Cell-free assay) 0.006 μM |
体外研究 | 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.103 ml | 10.514 ml | 21.027 ml |
5 mM | 0.421 ml | 2.103 ml | 4.205 ml |
10 mM | 0.21 ml | 1.051 ml | 2.103 ml |
5 mM | 0.042 ml | 0.21 ml | 0.421 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!