1. Immunology/Inflammation Apoptosis
  2. PD-1/PD-L1 Interleukin Related TNF Receptor
  3. Cetrelimab

Cetrelimab  (Synonyms: JNJ 63723283; JNJ 3283)

目录号: HY-P99499 纯度: 100.00%
COA

Cetrelimab (JNJ 63723283; JNJ 3283) 是一种靶向 PD-1 的人源 IgG4κ 单克隆抗体。Cetrelimab 结合 PD-1 的 Kd 为 1.72 nM (HEK293 细胞)。由此,Cetrelimab 阻断 PD-1PD-L1PD-L2 的相互作用 (IC50 分别为 111.7 ng/mL 和 138.6 ng/mL)。Cetrelimab 还刺激外周 T 细胞,增加细胞因子 (IFN-γ, IL-2, TNF-α) 水平,并抑制体内肿瘤生长。

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Cetrelimab Chemical Structure

Cetrelimab Chemical Structure

CAS No. : 2050478-92-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (Kd=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC50s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo[1].

IC50 & Target

PD-1/PD-L1, PD-1/PD-L2, IFN-γ, IL-2, and TNF-α[1]

体外研究
(In Vitro)

Cetrelimab (0.01-30 nM; 5 d) 在活化 CD4+ 和 CD8+ T 细胞上与内源性 PD-1 结合,EC50 分别为 0.16-0.22 µg/mL 和 0.17-0.22 µg/mL[1]
Cetrelimab (0.01-30 μg/mL; 24 h) 在表达 PD-L1 的 CHO-K1 的 Jurkat-PD-1 NFAT 报告细胞中逆转 PD-1 导致的 TCR 信号抑制[1]
Cetrelimab (0.001-100 nM; 6 d) 增加 IFN-γ,IL-2,和 TNF-α,EC50 分别为 0.08 ng/mL,0.07 ng/mL,和 0.02 ng/mL[1]
Cetrelimab 与猕猴来源的 PD-1 结合,Kd 值为 0.9 nM[1]

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

体内研究
(In Vivo)

Cetrelimab (10 mg/kg; 腹腔注射; 单剂量) 对带有 MC38 肿瘤的 PD-1 敲入 (hPD-1KI) 小鼠具有抗肿瘤作用,并能减小肿瘤体积[1]
Cetrelimab (10 mg/kg; 腹腔注射; 每 5 天 1 次, 共 30 天) 在患者源性异种移植 (PDX) 小鼠肺癌模型中,外周血 CD8+ T 细胞显著增加[1]
Cetrelimab (10-100 mg/kg; 静脉注射; 每周 1 次, 共 5 周) 在猕猴中具有良好的耐受性[1]
Cetrelimab (0.1-10 mg/kg; 静脉注射; 单剂量, 监测 57 天) 在猕猴中显示出非线性的药代动力学 (PK) 特征,可能归因于靶介导药物沉积 (TMDD)[1]

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

Animal Model: hPD-1KI model with mouse PD-1 ECD replaced by the human PD-1 ECD[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; single dose at day 7 after tumor implantation
Result: hPD-1KI mice develop normally and have no immune abnormalities.
Significantly lowered tumor volume at Day 21.
Animal Model: Patient-derived xenograft (PDX) LG1306 lung model in mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; every 5 days for 6 cycles
Result: Significantly reduced patient-derived tumor volume by 32%.
Animal Model: Good Laboratory Practice (GLP) toxicity study in cynomolgus[1]
Dosage: 0, 10, 30, or 100 mg/kg
Administration: Intravenous injection; once weekly for 5 weeks
Result: Showed well tolerance in cynomolgus.
Clinical Trial
CAS 号
性状

液体

颜色

Colorless to light yellow

运输条件

Shipping with dry ice.

储存方式

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

纯度 & 产品资料

纯度: 100.00%

参考文献
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  • 稀释计算器

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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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Cetrelimab
目录号:
HY-P99499
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