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Updated: Aug 22, 2026
Quantifying Antibody-Dependent Cellular Cytotoxicity in a Tumor Spheroid Model: Application for Drug Discovery
Published on: April 26, 2024
TZT-1027 elucidates antitumor activity through direct cytotoxicity and selective blockade of blood supply
Naoko Hashiguchi1, Tetsuro Kubota, Jun-Ichi Koh
1Department of Surgery, School of Medicine, Keio University, Tokyo 160-8582, Japan.
Background:
TZT-1027 is a newly developed antitumor agent derived from dolastatin 10.
Materials And Methods:
The in vitro activity of TZT-1027 on MCF-7 and R-27 cells was evaluated by MTT assay. TZT-1027 1 mg/kg/week was administered i.v. for 4 weeks into nude mice bearing MCF-7 and R-27. Subsequently, primary cultured cells from xenografts were also used for CD-DST. Two mg of TZT-1027 or 40 mg docetaxel per kg were injected i.v. into nude mice bearing R-27. 0.2% Evans blue was injected to assess the blood flow.
Results:
TZT-1027 suppressed the in vitro growth of MCF-7 cells, while R-27 cells were resistant to TZT-1027, although its in vivo antitumor activity was remarkable. TZT-1027 blockaded R-27 tumor blood flow immediately after injection; blood flow was not affected by docetaxel.
Conclusion:
TZT-1027 exerts its antitumor activity through direct cytotoxicity against MCF-7 cells and through selective blockade of tumor blood flow against R-27 cells.
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