货号:A121482 同义名: Programmed Cell Death 1/Programmed Cell Death-Ligand 1 Inhibitor 1;PD-1/PD-L1 inhibitor 1
BMS-1作为一种抑制剂,靶向PD-1/PD-L1蛋白-蛋白相互作用,IC50值在6到100 nM之间。
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产品名称 | PD-1 ↓ ↑ | PD-1/PD-L1 ↓ ↑ | PD-1/PD-L1 interaction ↓ ↑ | PD-L1 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SR0987 | ✔ | 98% | |||||||||||||||||
Pembrolizumab | ✔ | 98% | |||||||||||||||||
Camrelizumab | ✔ | 5mg/mL | |||||||||||||||||
Spartalizumab | ✔ | 95% | |||||||||||||||||
BMS-1001 |
+
PD-1/PD-L1, EC50: 253 nM |
+
PD-1/PD-L1, EC50: 253 nM |
98% | ||||||||||||||||
INCB086550 |
++
PD-1/PD-L1, IC50: <10 nM |
++
PD-1/PD-L1, IC50: <10 nM |
98% | ||||||||||||||||
BMS-1 |
++
PD-1/PD-L1 interaction, IC50: 0.006 μM |
99%+ | |||||||||||||||||
BMS-202 |
+
PD-1/PD-L1 interaction, IC50: 0.018 μM |
99%+ | |||||||||||||||||
PD-1/PD-L1-IN 3 |
+++
PD-1/PD-L1 interaction, IC50: 5.6 nM |
98+% | |||||||||||||||||
Nivolumab |
+++
PD-1/PD-L1 interaction, IC50: 2.52 nM |
95% | |||||||||||||||||
BMS-1166 |
+++
PD-1/PD-L1 interaction, IC50: 1.4 nM |
99%+ | |||||||||||||||||
Durvalumab |
++++
PD-1/PD-L1 interaction, IC50: 0.1 nM |
95% | |||||||||||||||||
Evixapodlin |
++++
PD-1/PD-L1, IC50: 0.213 nM |
95% | |||||||||||||||||
CA-170 | ✔ | 97% (contains 2.7% ethanol) | |||||||||||||||||
Atezolizumab |
+++
hPD-L1, Kd: 0.4 nM |
98% | |||||||||||||||||
AUNP-12 | ✔ | 99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | BMS-1 is a selective inhibitor targeting the interaction between PD-1 and PD-L1, with an inhibitory concentration range (IC50) spanning from 6 to 100 nM[1].[2]. |
体内研究 | BMS-1 (500 μg/mL; 100 μL; i.p.) markedly enhances the survival rates of the mVEGF165b group and mVEGF165b + MUC1 group[3]. |
体外研究 | BMS-1 is applied to disrupt the PD-1/PD-L1 engagement, a critical pathway in the exhaustion of natural killer (NK) cells, by directly inhibiting their interaction. Specifically, at a dosage of 1 μM over a period of three days, BMS-1 has been shown to counteract the dexamethasone-induced upregulation of PD-1 expression and the consequent reduction in cytotoxicity observed in co-cultured NK92 cells[1]. As a small-molecule inhibitor that impedes the PD-1/PD-L1 immune checkpoint, BMS-1 presents a viable option for therapeutic interventions in tumor immunotherapy[2]. |
Dose | Mice: 500 μg/mL, 100 μL[1] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.10mL 0.42mL 0.21mL |
10.51mL 2.10mL 1.05mL |
21.03mL 4.21mL 2.10mL |
CAS号 | 1675201-83-8 |
分子式 | C29H33NO5 |
分子量 | 475.576 |
别名 | Programmed Cell Death 1/Programmed Cell Death-Ligand 1 Inhibitor 1;PD-1/PD-L1 inhibitor 1;PD1-PDL1-IN1;PD1-PDL1 inhibitor 1 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 6 mg/mL(12.62 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO DMF: 5 mg/mL(10.51 mM),配合低频超声助溶 |
动物实验配方 |
IP 5% DMSO + water 0.1 mg/mL clear |