1. Immunology/Inflammation JAK/STAT Signaling Stem Cell/Wnt Epigenetics Protein Tyrosine Kinase/RTK
  2. PD-1/PD-L1 JAK
  3. PJ27

PJ27 是一种双重 PD-1/PD-L1/JAK1 抑制剂,其对 PD-1/PD-L1IC50 为 414 nM,对 JAK1 的 IC50 为 786 nM,对人源 PD-1/PD-L1Ka 为 294 nM,对小鼠源 PD-1/PD-L1Ka 为 473 nM。PJ27 可促进 CD3+CD8+CD3+CD4+ 细胞浸润至肿瘤微环境,具有显著的免疫激活作用。PJ27 在 LLC 肺癌小鼠模型中呈剂量依赖性抑制肿瘤生长。PJ27 可用于肺癌的相关研究。

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PJ27

PJ27 Chemical Structure

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Customer Review

查看 JAK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3+CD8+ and CD3+CD4+ cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer[1].

IC50 & Target

JAK3

786 nM (IC50)

体外研究
(In Vitro)

PJ27 (0.125-2 μM; 48 h) 可增强 Jurkat T 细胞对表达 PD-L1 的 A549 细胞的杀伤作用,共培养体系中 2 μM 浓度下 A549 细胞活力出现显著降低[1]
PJ27 与人源及鼠源 PD-L1 结合的亲和力相近,其 Kd 值分别为 294 nM 和 473 nM[1]

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

Cell Viability Assay[1]

Cell Line: A549, Jurkat T cells
Concentration: 0, 0.125, 0.25, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Showed almost no inhibitory activity against A549 or Jurkat T cells cultured alone.
Significantly decreased A549 cell viability at 2 μM in co-culture model.
Enhanced Jurkat T cell-mediated killing of A549 cells in co-culture model.
体内研究
(In Vivo)

PJ27 (25-50 mg/kg; i.p.; daily; 11 days) 可强效且呈剂量依赖性地抑制雄性 C57BL/6J 小鼠体内 LLC 肺癌的生长,在 50 mg/kg 剂量下的肿瘤生长抑制率达 56%,同时还能增强抗肿瘤 T 细胞的浸润,且未表现出明显毒性[1]

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

Animal Model: C57BL/6J (male, 5 to 6 weeks old, subcutaneous inoculation of 1 × 106 LLC cells)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.p.; daily; 11 days
Result: Achieved a tumor growth inhibition rate (TGI) of 21% and reduced phosphorylated STAT3 (p-STAT3) levels in tumor tissues compared to control at 25 mg/kg.
Achieved a TGI of 56%, reduced p-STAT3 and PD-L1 levels in tumor tissues, increased the percentage of CD3+CD8+ cytotoxic T cells in tumor tissues to 38.8% (vs.
16.3% in control), and increased the percentage of CD3+CD4+ helper T cells in tumor tissues to 50.5% (vs.
28.9% in control) at 50 mg/kg.
Showed no significant body weight loss or organ toxicity in either dose group.
分子量

640.78

Formula

C38H40N8O2

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)

质量   浓度   体积   分子量 *
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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:
PJ27
目录号:
HY-181663
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