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。

PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects[1].

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[1].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)[1].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[1].

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[1].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[1].PD-1/PD-L1-IN-NP19 (1 mg/kg; i.v.) shows the half time (t1/2=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[1].PD-1/PD-L1-IN-NP19 (10 mg/kg; p.o.) shows the oral absorption (Tmax=0.6±0.2 h), long half-life (t1/2=10.9±7.7 h) and oral bioavailability (F=5%) in rats[1].

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C33H31ClN2O4

555.06

PD-1/PD-L1-IN-NP19

DMSO:1.8 mg/mL (3.2 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years