Zaptuzumab  (Synonyms: AD5-10)

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]}.

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.

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.

8795  [NCBI]

2378046-35-4

N/A

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

• [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]