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。

PD-1/PD-L1-IN-9 is a potent and orally active inhibitor of PD-1/PD-L1 interaction, IC50 = 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.

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

PD-1/PD-L1-IN-9 (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. 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. 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].

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