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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C39H44ClN3O6
- 分子量:686.24
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
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) .
化学情報
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分子量 686.24
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)