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编 号：F748530
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规格
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1mg
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询价
5mg
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CAS No: 2050478-92-5
产品详情
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.
体内研究：
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。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。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。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)。Animal Model:hPD-1KI model with mouse PD-1 ECD replaced by the human PD-1 ECD
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
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
Dosage:0, 10, 30, or 100 mg/kg
Administration:Intravenous injection; once weekly for 5 weeks
Result:Showed well tolerance in cynomolgus.
体外研究：
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。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。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。Cetrelimab 与猕猴来源的 PD-1 结合，Kd 值为 0.9 nM。
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.
体内研究：
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。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。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。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)。Animal Model:hPD-1KI model with mouse PD-1 ECD replaced by the human PD-1 ECD
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
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
Dosage:0, 10, 30, or 100 mg/kg
Administration:Intravenous injection; once weekly for 5 weeks
Result:Showed well tolerance in cynomolgus.
体外研究：
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。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。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。Cetrelimab 与猕猴来源的 PD-1 结合，Kd 值为 0.9 nM。
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