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Zalutumumab

Names

[ CAS No. ]:
667901-13-5

[ Name ]:
Zalutumumab

Biological Activity

[Description]:

Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[In Vitro]

Zalutumumab (0-1 μM; 60 min) effectively blocks EGF-induced EGFR activation with an IC50 value of 1.3 nM[2]. Zalutumumab (0-1 μM; 96 h) affects proliferation of A431 cells[2]. Zalutumumab (10 μg/mL; 24 h) induces a comparable percentage of specificlysis of A431 cells with mouse macrophages[3]. Cell Proliferation Assay[2] Cell Line: A431 cell line Concentration: 0-1 μM Incubation Time: 96 hours Result: Inhibited A431 cells proliferation with an IC50 value of 1.5 nM.

[In Vivo]

Zalutumumab (5 mg/kg; i.p. 2 h after tumor induction) affects tumor growth in A431 xenograft models[3]. Zalutumumab (0.5 and 5 mg/kg; i.p. once ) delays tumor growth when mice with tumor volumes of 80-100 mm3[3]. Animal Model: SCID mice with A431 cells injection[3] Dosage: 5 mg/kg Administration: Intraperitoneal injection; 5 mg/kg 2 hours after tumor induction Result: Effectively inhibited tumor growth in A431 xenograft models with an early treatment.

[References]

[1]. Schick U, et al. Zalutumumab in head and neck cancer. Expert Opin Biol Ther. 2012 Jan;12(1):119-25.

[2]. Lammerts van Bueren JJ, et al. The antibody zalutumumab inhibits epidermal growth factor receptor signaling by limiting intra- and intermolecular flexibility. Proc Natl Acad Sci U S A. 2008 Apr 22;105(16):6109-14.

[3]. Overdijk MB, et al. Epidermal growth factor receptor (EGFR) antibody-induced antibody-dependent cellular cytotoxicity plays a prominent role in inhibiting tumorigenesis, even of tumor cells insensitive to EGFR signaling inhibition. J Immunol. 2011 Sep 15;187(6):3383-90.

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds