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PD-1/PD-L1-IN-9 hydrochloride

CAS No. :

MCE 站：PD-1/PD-L1-IN-9 hydrochloride

产品活性：PD-1/PD-L1-IN-9 盐酸盐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 盐酸盐可以增强免疫细胞对肿瘤细胞的杀伤活性。PD-1/PD-L1-IN-9 盐酸盐在 CT26 小鼠模型中表现出显着的体内抗肿瘤活性。

研究领域：Immunology/Inflammation

作用靶点：PD-1/PD-L1

In Vitro: PD-1/PD-L1-IN-9 hydrochloride (compound 24) (46.9-1500 nM; pretreated for 2 h) dose-dependently significantly activates the antitumor immunity of peripheral blood mononuclear cells (PBMCs) to MDB-MB 231 cells, with an EC₅₀ of 100 nM.

In Vivo: PD-1/PD-L1-IN-9 hydrochloride (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.
PD-1/PD-L1-IN-9 hydrochloride (3 mg/kg; i.v.; single dose) exhibits half-life (T_1/2=4.2 h), plasma clearance (Cl=11.5 L/h/kg) ａnd C_max (1233 ng/mL) in rats.
PD-1/PD-L1-IN-9 hydrochloride (25 mg/kg; p.o.; single dose) exhibits moderate oral bioavailability (F=22 %), half-life (t_1/2=6.4 h) ａnd C_max (192 ng/mL) in rats.

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