1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. NPH16

NPH16 是一种口服有效的 PD-1/PD-L1 抑制剂,其 IC50 为 2.24 nM。 NPH16 能促进 HepG2 细胞凋亡 (apoptosis)。NPH16 在体内表现出出色的抗肿瘤效果和良好的药代动力学特性。NPH16 可用于肝癌研究。

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NPH16 Chemical Structure

NPH16 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 2.24 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[1].

体外研究
(In Vitro)

NPH16 (0-2 μM, 48 h) 在细胞共培养体系中对 HepG2 细胞表现出剂量依赖性的细胞毒性[1]
NPH16 (0.02-20 μM, 0-700 s) 与人类 PD-L1(解离常数 KD = 54.6 nM)以及小鼠 PD-L1(解离常数 KD = 51.6 nM)以浓度依赖的方式相互作用[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG2, HepG2/Jurkat T cell coculture
Concentration: 0, 0.25, 0.5, 1, 2 μM
Incubation Time: 48 h
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.
体内研究
(In Vivo)

NPH16 (50-100 mg/kg, p.o., 7 天) 在携带 HEPA1-6 肝癌肿瘤的 C57BL/6 小鼠模型中,整个治疗期间展现出明显的剂量依赖性抗肿瘤活性[1]

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

Animal Model: C57BL/6 mice bearing HEPA1-6 hepatoma tumors[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: p.o., for 7 days
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) .
分子量

686.24

Formula

C39H44ClN3O6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
NPH16
目录号:
HY-174424
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