PD-1/PD-L1-IN-9 hydrochloride is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC 50 of 3.8 nM. PD-1/PD-L1-IN-9 hydrochloride can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 hydrochloride also exhibits significant in vivo antitumor activity in a CT26 mouse model.
性状
Solid
体外研究(In Vitro)
PD-1/PD-L1-IN-9 盐酸盐(compound 24) (46.9-1500 nM; 预处理 2 h) 剂量依赖性地激活外周血单核细胞 (PBMCs) 对 MDB-MB 231 细胞的抗肿瘤免疫,EC50 约为 100 nM。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PD-1/PD-L1-IN-9 盐酸盐 (化合物24) (40-80 mg/kg; 口服; 每天一次,持续 2 周) 以剂量依赖的方式抑制肿瘤生长,并且不会导致小鼠体重减轻或死亡。
PD-1/PD-L1-IN-9 盐酸盐 (3 mg/kg; 静脉注射; 单次剂量) 在大鼠中的半衰期 T 1/2 =4.2 h、血浆清除率 Cl=11.5 L/h/kg,C max =1233 ng/mL。
PD-1/PD-L1-IN-9 盐酸盐 (25 mg/kg; 口服; 单次剂量) 在大鼠中表现出中等的口服生物利用度 (F= 22%)、半衰期 (t 1/2 =6.4 h),和 C max (=192 ng/mL)。 has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Wang T, et, al. Novel Biphenyl Pyridines as Potent Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction. J Med Chem. 2021 May 30.
溶解度数据
In Vitro: DMSO : 125 mg/mL (324.76 mM; Need ultrasonic)配制储备液