PD-1/PD-L1-IN-9 是一种有效和具有口服活性的 PD-1/PD-L1 相互作用抑制剂，IC50 值为 3.8 nM。PD-1/PD-L1-IN-9 可以增强免疫细胞对肿瘤细胞的杀伤活性。PD-1/PD-L1-IN-9 在 CT26 小鼠模型中表现出显着的体内抗肿瘤活性。
货号:ajcx33622
CAS:2628506-54-5
分子式:C22H24N2O2
分子量：348.44
溶解度:DMSO : 100 mg/mL (286.99 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, with an IC50 of 3.8 nM. PD-1/PD-L1-IN-9 can enhance the killing activity of tumor cells by immune cells. PD-1/PD-L1-IN-9 also exhibits significant in vivo antitumor activity in a CT26 mouse model[1].

PD-1/PD-L1-IN-9 (compound 24) (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of PBMCs to MDB-MB 231 cells, with an EC50 of ∼100 nM[1].

PD-1/PD-L1-IN-9 (compound 24) (40-80 mg/kg; p.o. once a day for 2 weeks) inhibits tumor growth in a dose-dependent manner and does not cause any body weight loss or mortality of mice[1].PD-1/PD-L1-IN-9 (3 mg/kg; a single i.v.) exhibits half-life (t1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) and Cmax (1233 ng/mL) in rats[1].PD-1/PD-L1-IN-9 (25 mg/kg; a single p.o.) exhibits moderate oral bioavailability (F=22 %), half-life (t1/2=6.4 h) and Cmax (192 ng/mL) in rats[1].

[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.