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PD-1

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PD-1

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CAS No. 1675201-83-8

分子式 C29H33NO5

分子量 475.58

英文名称 2-Piperidinecarboxylic acid, 1-[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-, (2S)-

中文同义词 (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;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

基本信息

产品名称

PD-1

中文同义词

(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,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

T3655;(2S)-1-{2,6-Dimethoxy-4-[(2-methyl-3-biphenylyl)methoxy]benzyl}-2-piperidinecarboxylic acid;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;PD1-PDL1 inhibitor 1 (PD1-PDL1-IN1)

CAS No.

1675201-83-8

分子式

C29H33NO5

分子量

475.58

EINECS号

MDL NO.

MOL

1675201-83-8.mol

性质

密度

1.182±0.06 g/cm3(Predicted)

形态

固体

沸点

630.2±55.0 °C(Predicted)

颜色

白色

储存条件

-20°C

酸度系数(pKa)

2.34±0.20(Predicted)

溶解度

可溶于 DMSO（高达至少 25 mg/ml）或乙醇（高达 20 mg/ml）

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。

用途

靶点

TargetValue PD-1/PD-L1 interaction (Cell-free assay) 0.006 μM

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.

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.

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。

编辑结构

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