2. Apoptosis Autophagy PI3K/Akt/mTOR MAPK/ERK Pathway
  3. TNF Receptor Apoptosis Caspase Atg8/LC3 Akt Beclin1 JNK
  4. Zaptuzumab

Zaptuzumab (AD5-10) 是一种针对死亡受体 5 (DR5) 的人源化的单克隆抗体，对 DR5 具有选择性的高结合亲和力。Zaptuzumab 通过 caspase 介导的凋亡 (apoptosis) 和自噬性细胞死亡 (ACD)，特异性诱导癌细胞死亡。Zaptuzumab 可以激活抗体依赖的细胞介导的细胞毒性作用 (ADCC) 和补体依赖的细胞毒性作用 (CDC)。Zaptuzumab 可以诱导活性氧 (ROS) 产生并降低 谷胱甘肽 (GSH) 水平。Zaptuzumab 在多种异种移植小鼠肿瘤模型中显示出显著的抑制肿瘤生长的作用和良好的安全性[1][2][3][4][5]。

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Zaptuzumab Chemical Structure

Zaptuzumab Chemical Structure

CAS No. : 2378046-35-4

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Zaptuzumab 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Zaptuzumab (AD5-10) is a DR5-specific humanized monoclonal antibody that selectively binds to DR5 with high affinity. Zaptuzumab specifically induces cancer cell death by both caspase-apoptosis and autophagic cell death (ACD). Zaptuzumab activates both ADCC and CDC. Zaptuzumab induces ROS generation and GSH level reduction. Zaptuzumab shows a significant suppression of the tumor growth and good safety in various xenografts mice tumor models[1][2][3][4][5].

IC50 & Target

TNFRSF10B/TRAILR2/CD262
体外研究
(In Vitro)

Zaptuzumab (AD5-10) (0.01-10000 ng/mL, 48 h) 特异性杀死多种肿瘤细胞，但对正常细胞系无作用[3]。

Zaptuzumab (0.00001-10000 nM, 72 h) 对 Jurkat E6-1, Ju rkat, J.gamma1, Reh, A3, and MT-4 细胞显示出显著的细胞毒性[2]。

Zaptuzumab (5 μg/mL, 4 h) 可激活癌细胞中的抗体依赖的细胞介导的细胞毒性作用 (ADCC) 和补体依赖的细胞毒性作用 (CDC)[3]。

Zaptuzumab (20 μg/mL, 0.5-1.5 h) 通过内吞作用从 NCI-H460 细胞的质膜转移到细胞质区室[3]。

Zaptuzumab (1 μg/mL, 0.5-24 h) 通过下调磷酸化的 caspase-8, 9, and 3 的水平，诱导 NCI-H460 细胞凋亡[3]。

Zaptuzumab (0.1-1µg/mL) 以剂量依赖性方式NF-κB，并触发炎症细胞因子的释放，IL-8, TNF-α, CCL20, MIP-2 and MIP-1β[4]。

Zaptuzumab (40 ng/mL, 0-4 h) 可诱导 Jurkat 细胞产生活性氧 (ROS)，并降低谷胱甘肽 (GSH) 水平[5]。

Zaptuzumab (40 ng/mL, 0-4 h) 可降低 Jurkat 细胞的线粒体膜电位并氧化心磷脂[5]。

Zaptuzumab (40 ng/mL, 0.5-4 h) 可下调 Jurkat 细胞中 Bid、AIF、Endo G、procaspase-8 和 PARP 的水平[5]。

Zaptuzumab (40 ng/mL, 4 h) 可促使 Endo G 从 Jurkat 细胞和 HCT116 细胞的细胞质转移至细胞核[5]。

Zaptuzumab (40 ng/mL, 0-4 h) 可诱导 Jurkat 细胞中 JNK 的持续激活[5]。

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

Zaptuzumab 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Tumor cells of Jurkat E6-1, J.gamma1, A3, Reh; namoral cells
Concentration: 0, 0.01, 0.1, 1, 10, 100, 1,000 and 10000 ng/mL
Incubation Time: 48 h
Result: Killed tumor cells and shows good safety for normal cells.

Cell Cytotoxicity Assay[3]

Cell Line: Tumor cells of SMMC-7721, HCT116, A549, U251, MDA-MB-231, NCI-H460, Jurkat, and normal PBMCs
Concentration: 0, 0.094, 0.188, 0.375, 0.75, 1.5, 3.0 and 6.0 μg/mL
Incubation Time: 24 h
Result: Cell Cytotoxicity AssShowed ID50 values of the0.85 μg/mL (SMMC-7721), 0.10 μg/mL (HCT116), 1.08 μg/mL (A549), 0.34 μg/mL (U251), 2.72 μg/mL (MDA-MB-231), 0.14 μg/mL (NCI-H460), and 0.28 μg/mL (Jurkat), respectively.
Showed no toxicity in normal PBMCs.

Western Blot Analysis[3]

Cell Line: NCI-H460 cells
Concentration: 1 μg/mL
Incubation Time: 0.5, 1, 2, 4, 8, 12 and 24 h
Result: Showed the cleavages of procaspase-8, 9, and 3.
Markedly decreased LC3-I, p-AKT, p-IαBα levels and increased p-JNK, Beclin-1 expression.

RT-PCR[4]

Cell Line: 293T cells
Concentration: 0.1 and 1µg/mL
Incubation Time: /
Result: Triggered the inflammatory cytokine IL-8, TNF-α, CCL20, MIP-2 and MIP-1β release.

Western Blot Analysis[5]

Cell Line: Jurkat cells
Concentration: 40 ng/mL
Incubation Time: 0.5, 1, 2 and 4 h
Result: Downregulated the levels of Bid, procaspase-8 and its substrate PARP for 2 and 4 h.
Upregulated the levels of AIF and Endo G at 4 h.
体内研究
(In Vivo)

Zaptuzumab (AD5-10) (8 mg/kg；静脉注射；单次给药) 能够显著抑制 Reh, J. gamma1 和 Jurkat E6-1 异种移植瘤小鼠模型中肿瘤的生长[2]。

Zaptuzumab (40-80 mg/kg；腹腔注射；每周一次，持续四周) 能够抑制 NCI-H460 异种移植瘤小鼠模型中肿瘤的生长[3]。

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

Animal Model: Reh, J. gamma1 and Jurkat E6-1 xenografts mice models (BALB/c nude mice, tumor volume of 100-200 mm3)[2]
Dosage: 8 mg/kg
Administration: Intravenously injection; a single administration
Result: Showed a significant suppression of the tumor growth.
Animal Model: NCI-H460 xenografts mice models (BALB/c nude mice, female, 6 weeks, tumor volume of 90-100 mm3) [3]
Dosage: 40, 80 mg/kg, and 80 mg/kg with 4.5 mg/kg DDP (HY-17394)
Administration: Intraperitoneal injection, once a week for 4 weeks
Result: Showed the relative tumor growth inhibition, with TGI rates of 8.2% (40 mg/kg), 13.9% (80 mg/kg) and 66.1% (80 mg/kg with 4.5 mg/kg DDP), respectively.
Showed no toxicity to liver and kidney.
基因 ID

8795  [NCBI]

CAS 号
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

Zaptuzumab 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Zaptuzumab2378046-35-4AD5-10TNF ReceptorApoptosisCaspaseAtg8/LC3AktBeclin1JNKTumor Necrosis Factor ReceptorTNFRAutophagy-related 8PKBProtein kinase BAtg6c-Jun N-terminal kinaseDeath receptor 5 (DR5)ADCCCDCACDROSGSHCancerReh cellsNCI-H460 cellsInhibitorinhibitorinhibit

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