NPH16
NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer.
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- 화학식: C39H44ClN3O6
- 분자량:686.24
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
In Vitro
NPH16 (0-2 μM, 48 h) exhibits dose-dependent cytotoxicity against HepG2 cells in the coculture system[1].
NPH16 (0.02-20 μM, 0-700 s) interacts with human PD-L1 (KD = 54.6 nM) and mouse PD-L1 (KD = 51.6 nM) in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2, HepG2/Jurkat T cell coculture
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Concentration:0, 0.25, 0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Demonstrated low toxicity at 2 μM, with cell viability exceeding 98%.
Exhibited dose-dependent cytotoxicity in the coculture system.
Reduced cell viability to 58.7% in the HepG2/Jurkat coculture model.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice bearing HEPA1-6 hepatoma tumors[1]
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Dosage:50 mg/kg, 100 mg/kg
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Administration:Oral gavage (p.o.), for 7 days
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Result:Caused no significant weight loss or adverse reactions in the mice.
Demonstrated significant dose-dependent antitumor activity throughout the treatment period.
Reduced tumor weight and volume by 92.1% and 91.2%, respectively at a dose of 100 mg/kg.
Significantly decreased the tumor weight and volume, amounting to 77.5% and 74.8%, respectively at a dose of 50 mg/kg.
Maintained the cellular boundaries within the organ tissues distinct and no obvious cell necrosis observed.
Significantly reduced PD-L1 expression by approximately 40%.
Markedly elevated IFN-γ levels in tumor tissues (5.4-fold increase vs control) .
Increased the percentage of CD3+CD8+ cells (activated cytotoxic T cells) to 3.9% at a dose of 100 mg/kg.
Significantly reduced splenic Treg populations (0.7% vs 2.6% in vehicle controls), while producing a modest decrease in intratumoral Tregs at a dose of 100 mg/kg.
Substantially downregulated TIM3 protein expression relative to control groups(100 mg/kg) .
Chemical Information
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분자량 686.24
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화학식 C39H44ClN3O6
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SMILES
N#CC1=CC=CC(COC2=CC(OCC3=C(C(C4=CC(OCCOCCN5CC(CC5)O)=CC=C4)=CC=C3)C)=C(C=C2CNCCO)Cl)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)