1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. PD-1/PD-L1-IN-NP19

PD-1/PD-L1-IN-NP19 

Cat. No.: HY-131347
Handling Instructions

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.

For research use only. We do not sell to patients.

PD-1/PD-L1-IN-NP19 Chemical Structure

PD-1/PD-L1-IN-NP19 Chemical Structure

CAS No. : 2377916-66-8

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Description

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 & Target

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

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[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.

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[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].

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

Animal Model: BALB/c mice (6-8 weeks) with B16-F10 melanoma tumors[1]
Dosage: 25, 50, 100 mg/kg
Administration: Intragastric gavage once daily for 15 days
Result: Inhibited the growth of melanoma tumors up to 51.1, 75 and 80.9% at dose of 25, 50, 100 mg/kg, respectively.
Exhibited normal physical activity and increased body weights slightly.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: 1 mg/kg for i.v. and 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: I.v. and p.o.
Result: I.v.: t1/2=1.5 h; Cmax=1751 μg/L; CL=0.9 L/h/kg.
P.o.: t1/2=10.9 h; Cmax=69.5 μg/L; CL=23.1 L/h/kg.
Molecular Weight

555.06

Formula

C₃₃H₃₁ClN₂O₄

CAS No.

2377916-66-8

SMILES

CC(C)(NCC1=CC(Cl)=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)C=C1OCC4=CC=CC(C#N)=C4)C(O)=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PD-1/PD-L1-IN-NP19PD-1/PD-L1PD-1/Programmed death-ligand 1interactionimmunemicroenvironmenttumorcancerInhibitorinhibitorinhibit

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