Trastuzumab deruxtecan (solution) Chemical Structure
CAS No. : 1826843-81-5
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1mg (10 mg/mL * 100 μL in Aqueous solution)
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生物活性
Trastuzumab deruxtecan (DS-8201a) (solution) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan (solution) is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan (solution) can be used for the research of HER2-positive breast cancer and gastric cancer[1][2].
体外研究 (In Vitro)
Trastuzumab deruxtecan (1 pM-10 nM; 5 days) (solution) inhibits the growth of HER2-positive KPL-4 cells, with an IC50 of 109.7 pM[2]. Trastuzumab deruxtecan (10 nM; 5 days) (solution) shows bystander killing effects in HER2-negative MDA-MB-468 cells[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
KPL-4 and MDA-MB-468 cells
Concentration:
1, 10, 100, 1000, 10000 pM
Incubation Time:
5 days
Result:
Killed both HER2-positive KPL-4 cells and HER2-negative MDA-MB-468 cells.
体内研究 (In Vivo)
Trastuzumab deruxtecan (3 mg/kg; a single i.v.) (solution) shows antitumor activity against not only HER2-positive tumors but also HER2-negative tumors under the co-inoculated condition[2]. Trastuzumab deruxtecan (10 mg/kg; i.v. on days 0 and 7) (solution) inhibits the tumor growth in in EMT6-hHER2 syngeneic mouse model[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female BALB/c nude mice injected with NCI-N87 and MDA-MB-468-Luc cells[2]
Dosage:
3 mg/kg
Administration:
A single i.v.
Result:
Almost all of the HER2-positive and HER-negative cells disappeared and there were little or no cancer cells remaining in the tumors.
Clinical Trial
CAS 号
1826843-81-5
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Kotani D, et, al. Trastuzumab deruxtecan for the treatment of patients with HER2-positive gastric cancer. Ther Adv Med Oncol. 2021 Jan 7;13:1758835920986518.
[2]. Ogitani Y, et, al. Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity. Cancer Sci. 2016 Jul;107(7):1039-46.
[3]. Iwata TN, et, al. [Fam-] trastuzumab deruxtecan (DS-8201a)-induced antitumor immunity is facilitated by the anti-CTLA-4 antibody in a mouse model. PLoS One. 2019 Oct 1;14(10):e0222280.