Zaptuzumab
Based on 1 Customer Validation
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.
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- Pureza: 99.0%
- No. CAS: 2378046-35-4
- Peso molecular:144.86 kDa
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Human IgG1 kappa
Human
TNFRSF10B/TRAILR2/CD262
Zaptuzumab (AD5-10) (0-6 μg/mL, 24 h) specifically kills various types of tumor cells, but not normal cell lines[3].
Zaptuzumab (0.00001-10000 nM, 72 h) demonstrates significant cytotoxicity against Jurkat E6-1, Jurkat, J.gamma1, Reh, A3, and MT-4 cells[2].
Zaptuzumab (5 μg/mL, 4 h) activates both ADCC (antibodydependent cytotoxicity), CDC (complement-dependent cytotoxicity) and ACD (autophagic cell death) in NCI-H460 cells[3].
Zaptuzumab (20 μg/mL, 0.5-1.5 h) is translocated from the plasma membrane to the cytoplasmic compartments by endocytosis in NCI-H460 cells[3].
Zaptuzumab (1 μg/mL, 0.5-24 h) indues apoptosis by downregulating the levels of procaspase-8, 9, and 3 in NCI-H460 cells[3].
Zaptuzumab (0.1-1µg/mL) activates NF-κB in a dose-dependent manner and triggers the inflammatory cytokine release, such as IL-8, TNF-α, CCL20, MIP-2 and MIP-1β[4].
Zaptuzumab (40 ng/mL, 0-4 h) induces ROS generation and GSH level reduction in Jurkat cells[5].
Zaptuzumab (40 ng/mL, 0-4 h) decreases mitochondrial membrane potential and oxidize cardiolipin in Jurkat cells[5].
Zaptuzumab (40 ng/mL, 0.5-4 h) downregulates the levels of Bid, AIF and Endo G, procaspase-8 and its substrate PARP in Jurkat cells[5].
Zaptuzumab (40 ng/mL, 4 h) translocates Endo G from cytoplasm to nucleus in Jurkat and HCT116 cells[5].
Zaptuzumab (40 ng/mL, 0-4 h) induces sustained activation of JNK in Jurkat cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Tumor cells of Jurkat E6-1, J.gamma1, A3, Reh; namoral cells
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Concentration:0, 0.01, 0.1, 1, 10, 100, 1,000 and 10000 ng/mL
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Incubation Time:48 h
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Result:Killed tumor cells and showed good safety for normal cells.
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Cell Line:Tumor cells of SMMC-7721, HCT116, A549, U251, MDA-MB-231, NCI-H460, Jurkat, and normal PBMCs
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Concentration:0, 0.094, 0.188, 0.375, 0.75, 1.5, 3.0 and 6.0 μg/mL
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Incubation Time:24 h
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Result:Showed ID50 values of the 0.85 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.
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Cell Line:NCI-H460 cells
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Concentration:1 μg/mL
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Incubation Time:0.5, 1, 2, 4, 8, 12 and 24 h
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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.
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Cell Line:293T cells
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Concentration:0.1 and 1µg/mL
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Incubation Time:/
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Result:Triggered the inflammatory cytokine IL-8, TNF-α, CCL20, MIP-2 and MIP-1β release.
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Cell Line:Jurkat cells
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Concentration:40 ng/mL
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Incubation Time:0.5, 1, 2 and 4 h
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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.
Zaptuzumab (AD5-10) (8 mg/kg, i.v., a single dose) significantly suppresses tumor growth in Reh, J. gamma1 and Jurkat E6-1 xenografts mice models[2].
Zaptuzumab (40-80 mg/kg, i.p, once a week for 4 weeks) suppresses tumor growth in NCI-H460 xenografts mice models[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Reh, J. gamma1 and Jurkat E6-1 xenografts mice models (BALB/c nude mice, tumor volume of 100-200 mm3)[2]
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Dosage:8 mg/kg
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Administration:Intravenously injection; a single administration
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Result:Showed a significant suppression of the tumor growth.
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Animal Model:NCI-H460 xenografts mice models (BALB/c nude mice, female, 6 weeks, tumor volume of 90-100 mm3)[3]
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Dosage:40, 80 mg/kg, and 80 mg/kg with 4.5 mg/kg DDP (HY-17394)
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Administration:Intraperitoneal injection, once a week for 4 weeks
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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.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
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Immobilized Human TRAIL R2/DR5/TNFRSF10B Protein, His Tag can bind Zaptuzumab. The EC50 for this effect is 4.461 ng/mL. -
Flow cytometric analysis of 1X106 HepG2 cells labeling CD262 with Zaptuzumab (HY-P991570, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 for an hour at 4℃. AF488-conjugated Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa Isotype Control (HY-P99001, blue) was used as the isotype control.
Chemical Information
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No. CAS 2378046-35-4
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Appearance Liquid
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Peso molecular 144.86 kDa
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Color Colorless to light yellow
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SMILES
N/A
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Synonyms
AD5-10; oba-01 Antibody
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Envío
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Ficha de datos (268 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
Referencias
[1]. Zhang S, et al. A novel anti-DR5 antibody-drug conjugate possesses a high-potential therapeutic efficacy for leukemia and solid tumors. Theranostics. 2019 Jul 13;9(18):5412-5423. [Content Brief]
[2]. Zhang S, et al. Preclinical evaluation of a novel antibody-drug conjugate targeting DR5 for lymphoblastic leukemia therapy. Mol Ther Oncolytics. 2021 Apr 29;21:329-339. [Content Brief]
[3]. Chen L, et al. A novel humanized anti-tumor necrosis factor-related apoptosis-inducing ligand-R2 monoclonal antibody induces apoptotic and autophagic cell death. IUBMB Life. 2017 Sep;69(9):735-744. [Content Brief]
[4]. Tang W, et al. TRAIL receptor mediates inflammatory cytokine release in an NF-kappaB-dependent manner. Cell Res. 2009 Jun;19(6):758-67. [Content Brief]
[5]. Chen C, et al. An agonistic monoclonal antibody against DR5 induces ROS production, sustained JNK activation and Endo G release in Jurkat leukemia cells. Cell Res. 2009 Aug;19(8):984-95. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Zaptuzumab Related Classifications
HY-P991570 Related Classifications
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