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].

IC50: 12.5 nM (human PD-1/PD-L1)^[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 (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^[1].
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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

555.06

C₃₃H₃₁ClN₂O₄

2377916-66-8

固體

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. Cheng B, et, al. Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction As Potential Anticancer Agents. J Med Chem. 2020 Jul 15.  [Content Brief]