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PD-1/PD-L1-IN-NP19

CAS No. : 2377916-66-8

MCE 国际站：PD-1/PD-L1-IN-NP19

产品活性：PD-1/PD-L1-IN-NP19 是 PD-1/PD-L1 的抑制剂，抑制人类 PD-1/PD-L1 相互作用的 IC₅₀ 值为 12.5 nM。PD-1/PD-L1-IN-NP19 可以激活肿瘤的免疫微环境，这可能有助于其抗肿瘤作用。

研究领域：Immunology/Inflammation

作用靶点：PD-1/PD-L1

In Vitro: PD-1/PD-L1-IN-NP19 (compound NP19) (0.37-10 μM; 72 h) significantly elevates the production of IFN-γ in a dose dependent manner from T cells co-cultured with tumor cells.
PD-1/PD-L1-IN-NP19 exhibits much lower activity for inhibiting mouse PD-1/PD-L1 interaction with an IC₅₀ in the micromolar range (>1µM), as compared to the inhibition of human PD1/PD-L1 interaction (IC₅₀=12.5 nM).
PD-1/PD-L1-IN-NP19 (10 µM; 48 h) displays no apparent cytotoxic effects on A549, MCF-7, and B16-F10 cells at a concentration of 10 µM.

In Vivo: PD-1/PD-L1-IN-NP19 (compound NP19) (25-100 mg/kg; intragastric gavage once daily for 15 d) inhibits the growth of melanoma tumors dramatically in mice.
PD-1/PD-L1-IN-NP19 (25 mg/kg; i.p. daily for 14 d) demonstrates significant antitumor efficacy with a tumor growth inhibition (TGI) of 76.5% and is well tolerated in an H22 hepatoma mouse model.
PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) shows the half time (t_1/2=1.5±0.5 h), clearance rate (CL=0.9±0.2 L/h/kg) and apparent distribution volume (Vss=2.1±0.5 L/kg) in rats.
PD-1/PD-L1-IN-NP19 (10 mg/kg; p.o.) shows the oral absorption (T_max=0.6±0.2 h), long half-life (t_1/2=10.9±7.7 h) and oral bioavailability (F=5%) in rats.

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